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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

Product Citations (9)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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Flupirtine maleate

Catalog No. A10251
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NMDA 拮抗剂

Flupirtine maleate是Flupirine的盐形式，是一种非阿片类中枢性镇痛药，是一种选择性的神经元钾离子通道开放剂，也具有NMDA受体拮抗剂特性。了解更多

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Ostarine (MK-2866, GTx-024)

Catalog No. A10253
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Androgen Receptor Modulators

Ostarine (MK-2866,GTX-024)是一种雄激素受体调节剂(SARM)。了解更多

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ABT-737

Catalog No. A10255
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Bcl-2 抑制剂

ABT-737是一种类BH3抑制剂，能同时抑制Bcl-xL，Bcl-2和Bcl-w，EC50分别为78.7 nM，30.3 nM和197.8 nM;但对Mcl-1，Bcl-B及Bfl-1没有抑制作用。了解更多

Product Citations (15)

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- Jung Mo Lee, .et al. ABT-737, a BH3 Mimetic, Enhances the Therapeutic Effects of Ionizing Radiation in K-ras Mutant Non-Small Cell Lung Cancer Preclinical Model, Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. Utilizing in vitro drug release assays to predict in vivo drug retention in micelles, Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. OAS1/RNase L executes RIG-I ligand-dependent tumor cell apoptosis, Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. Invariant natural killer T cells coordinate removal of senescent cells, Med, 2021, 2,1-13
- Ying Ji, .et al. Use of ratiometrically designed nanocarrier targeting CDK4/6 and autophagy pathways for effective pancreatic cancer treatment, Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. The senotherapeutic drug ABT-737 disrupts aberrant p21 expression to restore liver regeneration in adult mice, Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. Inhibition of USP9X Downregulates JAK2-V617F and Induces Apoptosis Synergistically With BH3 Mimetics Preferentially in Ruxolitinib-Persistent JAK2-V617F-Positive Leukemic Cells, Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. α7-Nicotine acetylcholine receptor mediated nicotine induced cell survival and cisplatin resistance in oral cancer, Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. Lysophosphatidic acid promotes survival of T lymphoma cells by altering apoptosis and glucose metabolism, Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. Stem cell senescence drives age-attenuated induction of pituitary tumours in mouse models of paediatric craniopharyngioma, Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. Sorafenib targets the mitochondrial electron transport chain complexes and ATP synthase to activate the PINK1-Parkin pathway and modulate cellular drug response, J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. ABT-737 Synergizes with Cisplatin Bypassing Aberration of Apoptotic Pathway in Non-small Cell Lung Cancer, Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. Critical contribution of MCL-1 in EMT-associated chemo-resistance in A549 non-small cell lung cancer, Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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PD0325901

Catalog No. A10256
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MEK 抑制剂

PD0325901是一种选择性的，非ATP竞争性MEK抑制剂，无细胞试验中IC50为0.33 nM，对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。了解更多

Product Citations (5)

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- Jan Langkabel, .et al. Induction of peri-implantation stage synthetic embryos using reprogramming paradigms in ESCs, bioRxiv, 2021, January 25
- Ryan Clarke, .et al. Sequential Activation of Guide RNAs to Enable Successive CRISPR-Cas9 Activities, Mol Cell, 2021, Jan 21;81(2):226-238.e5 PMID: 33378644
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fukumoto S, .et al. Synergistic anti-proliferative effects of mTOR and MEK inhibitors in high-grade chondrosarcoma cell line OUMS-27, Acta Histochem, 2018, Feb;120(2):142-150 PMID: 29397960
- Yoshiteru Yano, .et al. Non-neural and cardiac differentiating properties of Tbx6-expressing mouse embryonic stem cells, Regenerative Therapy, 2016, 3 (2016) 1-6
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GDC-0449 (Vismodegib)

Catalog No. A10258
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Hedgehog 拮抗剂

GDC-0449 (Vismodegib)是一种新型有效的，特异性hedgehog抑制剂，IC50为3 nM。了解更多

Product Citations (3)

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Yi Yang, .et al. Tumidulin, a Lichen Secondary Metabolite, Decreases the Stemness Potential of Colorectal Cancer Cells, Molecules, 2018, Nov; 23(11): 2968 PMID: 30441806
- Olesen UH, .et al. Topical delivery of vismodegib using ablative fractional laser and micro-emulsion formulation in vitro, Lasers Surg Med, 2018, Aug 28 PMID: 30152536
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Imatinib (Gleevec)

Catalog No. A10259
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PDGFR 抑制剂

Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂，抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6，0.1和0.1 μM。了解更多

Product Citations (6)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Takafumi Shima, .et al. Glucose transporter-1 inhibition overcomes imatinib resistance in gastrointestinal stromal tumor cells, Oncol Rep, 2022, 47: 7 PMID: 34738628
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- BM Duggan, .et al. RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice, Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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ABT-263 (Navitoclax)

Catalog No. A10022
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Bcl-2 抑制剂

ABT-263 (Navitoclax)是一种有效的Bcl-2家族抑制剂 (Bcl-2，Bcl-xL和Bcl-w的Ki <1 nmol/L)。ABT-263对Bcl- xL，Bcl-2和Bcl-w，( Ki≤1nmol/ L) 维持高亲和力，但与Mcl-1和A1的结合更弱。了解更多

Product Citations (20)

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- Rindert Missiaen, .et al. GCN2 inhibition sensitizes arginine-deprived hepatocellular carcinoma cells to senolytic treatment, Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. Characterization of radiation-induced micronuclei associated with premature senescence, and their selective removal by senolytic drug, ABT-263, Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. Predicting and affecting response to cancer therapy based on pathway-level biomarkers, Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Hiroki Akiyama, .et al. Inhibition of USP9X Downregulates JAK2-V617F and Induces Apoptosis Synergistically With BH3 Mimetics Preferentially in Ruxolitinib-Persistent JAK2-V617F-Positive Leukemic Cells, Cancers, 2020, 12 (2) PMID: 32050632
- Stephanie Ketterer, .et al. Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling, Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. Clearance of HIV infection by selective elimination of host cells capable of producing HIV, Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Anderson R, .et al. Length-independent telomere damage drives postmitotic cardiomyocyte senescence, EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259
- Shinya Ishida, .et al. Mechanisms for mTORC1 activation and synergistic induction of apoptosis by ruxolitinib and BH3 mimetics or autophagy inhibitors in JAK2-V617F-expressing leukemic cells including newly established PVTL-2, Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488
- Rhys Anderson, .et al. Length-independent telomere damage drives cardiomyocyte senescence, bioRxiv, 2018, 2018
- Ryuta Mikawa, .et al. Elimination of p19ARF?\expressing cells protects against pulmonary emphysema in mice, Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Wei TW, .et al. Aurora A and NF-κB Survival Pathway Drive Chemoresistance in Acute Myeloid Leukemia via the TRAF-Interacting Protein TIFA, Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
- Yusuke Takagi, .et al. SPIB is a novel prognostic factor in diffuse large B?\cell lymphoma that mediates apoptosis via the PI3K-AKT pathway, Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272
- Matsumoto M, .et al. Cisplatin-induced apoptosis in non-small-cell lung cancer cells is dependent on Bax- and Bak-induction pathway and synergistically activated by BH3-mimetic ABT-263 in p53 wild-type and mutant cells, Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
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MDV3100

Catalog No. A10562
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Androgen receptor 拮抗剂

MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。了解更多

Product Citations (3)

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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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Obatoclax mesylate (GX15-070)

Catalog No. A10665
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Bcl-2 抑制剂

Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，拮抗所有抗凋亡Bcl-2家族蛋白（平均IC50，3 umol/L），包括Mcl-1（IC50，2.9 umol/L）和Bfl-1（IC50，5 umol/L）。了解更多

Product Citations (4)

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- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Silva S, .et al. A diarylamine derived from anthranilic acid inhibits ZIKV replication, Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
- Chi-Hung R. Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells, Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
- P Geserick, .et al. The ratio of Mcl-1 and Noxa determines ABT737 resistance in squamous cell carcinoma of the skin, Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
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Vandetanib (ZD6474)

Catalog No. A10963
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VEGFR 抑制剂

Vandetanib (ZD6474)是一种VEGFR和EGFR拮抗剂，是一种酪氨酸激酶抑制剂，对于HUVEC增殖，PC-9细胞和酪氨酸激酶活性，IC50为60、90、40 nM。了解更多

Product Citations (9)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Shinya Kitamura, .et al. Vandetanib inhibits cell growth in EGFR-expressing cutaneous squamous cell carcinoma, Biochem Biophys Res Commun, 2020, Aug 13 PMID: 32800552
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Rintaro Sogawa, .et al. Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib, JPA, 2018, in Press PMID: 30740257
- Park K, .et al. Vascular endothelial growth factor receptor 1 (VEGFR1) tyrosine kinase signaling facilitates granulation tissue formation with recruitment of VEGFR1+ cells from bone marrow, Anat Sci Int, 2018, Jun;93(3):372-383 PMID: 29256114
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Park K, .et al. Vascular endothelial growth factor receptor-1 (VEGFR-1) signaling enhances angiogenesis in a surgical sponge model, Biomed Pharmacother, 2016, Mar;78:140-149 PMID: 26898435
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RO4929097

Catalog No. A10802
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Gamma-secretase 抑制剂

RO4929097是一种γ secretase抑制剂，无细胞试验中IC50为4 nM。抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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PF-2341066 (Crizotinib)

Catalog No. A10712
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ALK/ c-Met 抑制剂

PF-2341066 (Crizotinib)是c-Met激酶和NPM-ALK的抑制剂。PF-2341066抑制ALK阳性ALCL细胞中的细胞增殖（IC50 = 30 nM）。了解更多

Product Citations (6)

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yu B, .et al. Pharmacokinetics and metabolism of ulixertinib in rat by liquid chromatography combined with electrospray ionization tandem mass spectrometry, J Sep Sci, 2020, Jan 22 PMID: 31970927
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Saki Omote, .et al. Effect of tyrosine kinase inhibitors on renal handling of creatinine by MATE1, Sci Rep, 2018, 8: 9237 PMID: 29915248
- Arakawa H, .et al. Inhibitory Effect of Crizotinib on Creatinine Uptake by Renal Secretory Transporter OCT2, J Pharm Sci, 2017, Sep;106(9):2899-2903 PMID: 28336299
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MS-275 (Entinostat)

Catalog No. A10611
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HDAC 抑制剂

MS-275 (Entinostat)是一种有效的HDAC抑制剂，对HDAC1和HDAC3的IC50分别为0.3和8uM。了解更多

Product Citations (5)

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- Vivek Bora, .et al. Systemic study of selected histone deacetylase inhibitors in cardiac complications associated with cancer cachexia, Can J Physiol Pharmacol, 2021, 6 October
- Taito Kashio, .et al. HDAC inhibitor, MS-275, increases vascular permeability by suppressing Robo4 expression in endothelial cells, Tissue Barriers, 2021, May 6;1911195 PMID: 33955828
- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- Arshdeep Singh, .et al. CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition, Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Minoru Ueda, .et al. The Distinct Roles of Class I and II RPD3-Like Histone Deacetylases in Salinity Stress Response, Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
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PTC124 (Ataluren)

Catalog No. A10758
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CFTR 抑制剂

PTC124也称为Ataluren，是CFTR-G542X无意义等位基因抑制剂。了解更多

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- L Kadunc, .et al. Increased Gene Translation Stringency in Mammalian Cells by Nonsense Suppression at Multiple Permissive Sites With a Single Noncanonical Amino Acid, FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. A flow cytometry-based reporter assay identifies macrolide antibiotics as nonsense mutation read-through agents, J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

Product Citations (12)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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MK-2206 2HCl

Catalog No. A10003
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AKT 抑制剂

MK-2206 2HCl是Akt1/2/3的高选择性抑制剂，IC50分别为8 nM/12 nM/65 nM。了解更多

Product Citations (17)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Ali Nasrollahzadeh, .et al. Anti-proliferative activity of disulfiram through regulation of the AKT-FOXO axis: A proteomic study of molecular targets, Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. Ultradian rhythms of AKT phosphorylation and gene expression emerge in the absence of the circadian clock components Per1 and Per2, PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Rosell??-Busquets, .et al. Nystatin Regulates Axonal Extension and Regeneration by Modifying the Levels of Nitric Oxide, Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. Chronic Activation of Gp1 mGluRs Leads to Distinct Refinement of Neural Network Activity Through Non-Canonical p53 and Akt Signaling, eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. Anti-apoptotic activity of human matrix metalloproteinase-2 attenuates diabetes mellitus, Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. Profiling the surface proteome identifies actionable biology for TSC1 mutant cells beyond mTORC1 signaling, bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. The O-glycosylating enzyme GALNT2 suppresses the malignancy of gastric adenocarcinoma by reducing EGFR activities, Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. Akt activation by Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) in ovarian cancer cells, J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. Constitutive activation of p46JNK2 is indispensable for C/EBPδ induction in the initial stage of adipogenic differentiation, Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. Periostin in tumor microenvironment is associated with poor prognosis and platinum resistance in epithelial ovarian carcinoma, Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. Inhibition of IL-1R1/MyD88 signalling promotes mesenchymal stem cell-driven tissue regeneration, Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. The tumor suppressor p53 guides GluA1 homeostasis through Nedd4-2 during chronic elevation of neuronal activity., J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624
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MLN8237 (Alisertib)

Catalog No. A10004
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Aurora A Kinase 抑制剂

MLN8237 (Alisertib)是一种选择性Aurora A抑制剂，在无细胞分析中的IC50为1.2 nM。它对Aurora A的选择性比Aurora B高200倍以上。了解更多

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- Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Kimura M, .et al. Aurora A regulates the architecture of the Golgi apparatus, Exp Cell Res, 2018, Jun 1;367(1):73-80 PMID: 29571950
- Jing Wang, .et al. The Aurora-A-Twist1 axis promotes highly aggressive phenotypes in pancreatic carcinoma, J Cell Sci, 2017, Mar 15; 130(6): 1078-1093 PMID: 28167680
- Lessing D, .et al. A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation, Proc Natl Acad Sci U S A, 2016, Dec 13;113(50):14366-14371 PMID: 28182563
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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(-)-Epigallocatechin gallate

Catalog No. A10005
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Antioxidant, antiangiogenic, antitumor agent

(-)-Epigallocatechin gallate是一种从绿茶中分离出来的强效抗氧化剂多酚类黄酮。了解更多

Product Citations (4)

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- Wafa Dridi, .et al. Influence of polysaccharide concentration on polyphenol-polysaccharide interactions, Carbohydr Polym, 2021, 274:118670 PMID: 34702486
- A S D'Costa, .et al. Inhibition of starch digestion by flavonoids: Role of flavonoid-amylase binding kinetics, Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Fenteany G, .et al. Multilevel structure-activity profiling reveals multiple green tea compound families that each modulate ubiquitin-activating enzyme and ubiquitination by a distinct mechanism, Sci Rep, 2019, Sep 5;9(1):12801 PMID: 31488855
- LiliSun, .et al. Comparative Effect of Black, Green, Oolong and White Tea Intake on Body Weight Gain and Bile Acid Metabolism, Nutrition, 2019, pii:S0899-9007(18)31140-7
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(-)-Huperzine A

Catalog No. A10006
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GluR 抑制剂

(-)-Huperzine A是一种天然存在的倍半萜生物碱化合物，存在于石楠石杉中。了解更多

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- Takuya Ohba, .et al. Protective effects of Huperzia serrata and its components against oxidative damage and cognitive dysfunction, PharmaNutrition, 2020, 13:100203
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LY294002

Catalog No. A10547
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PI3K 抑制剂

LY294002是PI3k抑制剂（IC50约为10μM）和酪蛋白激酶II抑制剂。了解更多

Product Citations (7)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Chien-Feng Li, .et al. EMP2 induces cytostasis and apoptosis via the TGF β/SMAD/SP1 axis and recruitment of P2RX7 in urinary bladder urothelial carcinoma, Cell Oncol (Dordr), 2021, Aug 2 PMID: 34339014
- Hiroharu Sakai, .et al. BRAP2 inhibits the Ras/Raf/MEK and PI3K/Akt pathways in leukemia cells, thereby inducing apoptosis and inhibiting cell growth, Exp Ther Med, 2021, March 5 PMID: 33747195
- Cheng Zhou, .et al. GLI1 reduces drug sensitivity by regulating cell cycle through PI3K/AKT/GSK3/CDK pathway in acute myeloid leukemia, Cell Death Dis, 2021, Mar 3;12(3):231 PMID: 33658491
- Daniel Limonta, .et al. Fibroblast growth factor 2 enhances Zika virus infection in human fetal brain, J Infect Dis, 2019, 2019 PMID: 30799482
- Lv H, .et al. CXCL8 gene silencing promotes neuroglial cells activation while inhibiting neuroinflammation through the PI3K/Akt/NF-κB-signaling pathway in mice with ischemic stroke, J Cell Physiol, 2018, Oct 26 PMID: 30362547
- Hui Liang, .et al. Targeting the PI3K/AKT pathway via GLI1 inhibition enhanced the drug sensitivity of acute myeloid leukemia cells, Sci Rep, 2017, 7: 40361 PMID: 28098170
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AC220 (Quizartinib)

Catalog No. A10027
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FLT3 抑制剂

AC220 (Quizartinib)是一种有效的选择性FLT3抑制剂，对于MC4-11和A375，IC50分别为0.56±0.3 nM和> 10 mM。了解更多

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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691. PMID: 25326874
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AZD8055

Catalog No. A10114
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mTOR 抑制剂

AZD8055是一种有效的，选择性的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM。了解更多

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- L. M. C. Koene, .et al. Effects of antiepileptic drugs in a new TSC/mTOR-dependent epilepsy mouse model, ACTN, 2019, June PMID: 31353861
- Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877–31888 PMID: 26397134
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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BEZ235 (NVP-BEZ235, Dactolisib)

Catalog No. A10133
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PI3K/mTOR 抑制剂

BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。了解更多

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- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
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YM155 (Sepantronium Bromide)

Catalog No. A11002
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Survivin 抑制剂

YM155 (Sepantronium Bromide)是一种新型小分子存活蛋白抑制剂，IC50为0.54 nM，可抑制存活蛋白启动子活性。了解更多

Product Citations (11)

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- Ali Nasrollahzadeh, .et al. Anti-proliferative activity of disulfiram through regulation of the AKT-FOXO axis: A proteomic study of molecular targets, Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Chia-Hui Huang, .et al. Arsenic Trioxide-Induced p38 MAPK and Akt Mediated MCL1 Downregulation Causes Apoptosis of BCR-ABL1-positive Leukemia Cells, Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
- Turner TH, .et al. Identification of synergistic drug combinations using breast cancer patient-derived xenografts, Sci Rep, 2020, Jan 30;10(1):1493 PMID: 32001757
- Chiou JT, .et al. Autophagic HuR mRNA degradation induces survivin and MCL1 downregulation in YM155-treated human leukemia cells, Toxicol Appl Pharmacol, 2019, Dec 16;387:114857 PMID: 31837377
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Yamamoto M, .et al. AS602801 Sensitizes Ovarian Cancer Stem Cells to Paclitaxel by Down-regulating MDR1, Anticancer Res, 2019, Feb;39(2):609-617 PMID: 30711936
- V??zquez-Mellado MJ, .et al. Erythropoietin promotes expression of survivin via STAT3 activation and reduces sensitivity to cisplatin in cervical cancer cells, Oncol Rep, 2018, Nov 27 PMID: 30483799
- MASAHIRO YAMAMOTO, .et al. AS602801, an Anticancer Stem Cell Candidate Drug, Reduces Survivin Expression and Sensitizes A2780 Ovarian Cancer Stem Cells to Carboplatin and Paclitaxel, Anticancer Res, 2018, Dec 38 (12) 6699-6706 PMID: 30504379
- Ahn MR, .et al. Both triazolyl ester of ketorolac (15K) and YM155 inhibit the embryonic angiogenesis in ovo (fertilized eggs) via their common PAK1-survivin/VEGF signaling pathway, Drug Discov Ther, 2017, 11(6):300-306 PMID: 29332887
- MASAYA MINODA, .et al. Antitumor effect of YM155, a novel small-molecule survivin suppressant, via mitochondrial apoptosis in human MFH/UPS, Int J Oncol, 2015, Sep; 47(3): 891-899 PMID: 26166250
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AZD1480

Catalog No. A10110
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JAK 抑制剂

AZD1480是一种新型有效的小型JAK2抑制剂，IC50为0.26 nM。了解更多

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- Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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Ibuprofen (Advil)

Catalog No. A10461
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COX-1 抑制剂

Ibuprofen (Advil)是一种非甾体抗炎药(NSAID)，靶向COX-1，IC50为13 μM。了解更多

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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Hesperadin

Catalog No. A10448
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Aurora B Kinase 抑制剂

Hesperadin是一种人极光B抑制剂，IC50为40 nM，用于防止底物磷酸化。它显著降低AMPK、Lck、MKK1、MAPKAP-K1、CHK1和PHK的活性，而不抑制MKK1在体内的活性。了解更多

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- Wenbin Ji, .et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases, PLoS One, 2016, 11(4): e0153518 PMID: 27082996
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SP600125

Catalog No. A10860
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JNK 抑制剂

SP600125是一种JNK抑制剂，对于JNK-1和JNK-2，IC50 = 40 nM，对于JNK-3，IC50 = 90 nM。了解更多

Product Citations (7)

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- Tetsuya Kouno, .et al. Selective PPARδ agonist seladelpar suppresses bile acid synthesis by reducing hepatocyte CYP7A1 via the fibroblast growth factor 21 signaling pathway, J Biol Chem, 2022, Jul;298(7):102056 PMID: 35605662
- Mark P Roberto, .et al. Mutations in the transcription factor FOXO1 mimic positive selection signals to promote germinal center B cell expansion and lymphomagenesis, Immunity, 2021, Aug 10;54(8):1807-1824.e14 PMID: 34380064
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Yuki Haga, .et al. Overexpression of c-Jun contributes to sorafenib resistance in human hepatoma cell lines, PLoS One, 2017, 12(3): e0174153 PMID: 28323861
- Jia-Shiuan Tsai, .et al. Cadmium Activates Multiple Signaling Pathways That Coordinately Stimulate Akt Activity to Enhance c-Myc mRNA Stability, PLoS One, 2016, 11(1): e0147011 PMID: 26751215
- Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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Axitinib

Catalog No. A10103
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VEGFR 抑制剂

Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。了解更多

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- Youcef M. Rustum, .et al. Non-Coding Micro RNAs and Hypoxia-Inducible Factors Are Selenium Targets for Development of a Mechanism-Based Combination Strategy in Clear-Cell Renal Cell Carcinoma-Bench-to-Bedside Therapy, Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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SRT1720 HCl

Catalog No. A10862
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SIRT1 Activator

SRT1720 HCl是一种抑制剂，旨在作为瑟土因亚型SIRT1的小分子活化剂。了解更多

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- Eleni Pitsillou, .et al. Interaction of small molecules with the SARS-CoV-2 main protease in silico and in vitro validation of potential lead compounds using an enzyme-linked immunosorbent assay, Comput Biol Chem, 2020, 89: 107408 PMID: 33137690
- Jie Ren, .et al. Melatonin prevents chronic intermittent hypoxia-induced injury by inducing sirtuin 1-mediated autophagy in steatotic liver of mice, Sleep Breath, 2018, Nov 8 PMID: 30411173
- Rowlands BD, .et al. Acetate metabolism does not reflect astrocytic activity, contributes directly to GABA synthesis, and is increased by silent information regulator 1 activation, J Neurochem, 2017, Mar;140(6):903-918 PMID: 27925207
- Adam Khader, .et al. SRT1720, a sirtuin 1 activator, attenuates organ injury and inflammation in sepsis, J Surg Res, 2017, Nov;219:288-295 PMID: 29078895
- Adam Khader, .et al. Sirtuin 1 Stimulation Attenuates Ischemic Liver Injury and Enhances Mitochondrial Recovery and Autophagy, Crit Care Med, 2016, Aug; 44(8): e651-e663 PMID: 26963320
- Benjamin D. Rowlands, .et al. Silent information regulator 1 modulator resveratrol increases brain lactate production and inhibits mitochondrial metabolism, whereas SRT1720 increases oxidative metabolism., J Neurosci Res., 2015, Jul;93(7):1147-56 PMID: 25677687
- Khader A, .et al. Sirtuin 1 activation stimulates mitochondrial biogenesis and attenuates renal injury after ischemia-reperfusion., Transplantation, 2014, 98(2):148-56 PMID: 24918615
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Pelitinib (EKB-569)

Catalog No. A10706
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EGFR 抑制剂

Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM 了解更多

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- Shi P, .et al. The Third-Generation EGFR Inhibitor, Osimertinib, Promotes c-FLIP Degradation, Enhancing Apoptosis Including TRAIL-Induced Apoptosis in NSCLC Cells with Activating EGFR Mutations, Transl Oncol, 2019, Mar 8;12(5):705-713 PMID: 30856555
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PD 0332991 HCl (Palbociclib)

Catalog No. A10701
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CDK 4/6 抑制剂

PD 0332991 HCl (Palbociclib)是一种高度选择性的CDK4/6抑制剂，它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性，具有潜在的抗肿瘤活性。了解更多

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- Hiroki Ozawa, .et al. Targeting AURKA in treatment of peritoneal tumor dissemination in gastrointestinal cancer, Transl Oncol, 2022, Feb;16:101307 PMID: 34902741
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Pirita Pekkonen, .et al. KSHV viral cyclin interferes with T-cell development and induces lymphoma through Cdk6 and Notch activation in vivo, Cell Cycle, 2014, Dec 1; 13(23): 3670-3684 PMID: 25483078
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Perifosine (NSC-639966)

Catalog No. A10709
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Akt 抑制剂

Perifosine (也为KRX-0401) 充当Akt抑制剂和PI3K抑制剂。了解更多

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- Bjune K, .et al. Inhibitors of AKT kinase increase LDL receptor mRNA expression by two different mechanisms, PLoS One, 2019, Jun 19;14(6):e0218537 PMID: 31216345
- Kyoung-Jae Won, .et al. Stability of the cancer target DDIAS is regulated by the CHIP/HSP70 pathway in lung cancer cells, Cell Death Dis, 2017, Jan; 8(1): e2554 PMID: 28079882
- Zhipeng Li, .et al. A positive feedback loop involving EGFR/Akt/mTORC1 and IKK/NF-κB regulates head and neck squamous cell carcinoma proliferation, Oncotarget, 2016, May 31; 7(22): 31892–31906 PMID: 26895469
- Won KJ, .et al. NSC126188 induces apoptosis of prostate cancer PC-3 cells through inhibition of Akt membrane translocation, FoxO3a activation, and RhoB transcription., Apoptosis., 2014, Jan;19(1):179-90 PMID: 24085402
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Neratinib (HKI-272)

Catalog No. A10638
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HER2 抑制剂

Neratinib (HKI-272)是一种酪氨酸激酶抑制剂。了解更多

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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FTY720 (Fingolimod)

Catalog No. A10408
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S1P Receptor 拮抗剂

FTY720 (Fingolimod)是ISP-1(肉豆蔻酸)的衍生物，ISP-1是中国草药Iscaria sinclarii的真菌代谢物，也是鞘氨醇的结构类似物。了解更多

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- Tina Sepasi, .et al. Targeted gene delivery to the brain using CDX-modified chitosan nanoparticles, BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. Effects of immunomodulatory drug Fingolimod (FTY720) on Chlamydia dissemination and pathogenesis, Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. Inulooligosaccharides in Atractylodis lanceae rhizoma and Atractylodis rhizoma of hochuekkito formula are essential for regulation of the pulmonary immune system of immuno-compromised mice, Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. 14-3-3 signal adaptor and scaffold proteins mediate GPCR trafficking, Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. Peyer's patch-immunomodulating glucans from sugar cane enhance protective immunity through stimulation of the hemopoietic system, Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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XL184 free base (Cabozantinib)

Catalog No. A10996
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VEGFR 抑制剂

XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶（特别是MET和VEGFR2）的小分子。了解更多

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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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MLN9708

Catalog No. A10602
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Proteasome 抑制剂

MLN9708是一种蛋白酶体抑制剂，可抑制蛋白酶体的活性，从而阻断通常由蛋白酶体进行的靶向蛋白水解。了解更多

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Flavopiridol (Alvocidib)

Catalog No. A10390
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CDK 抑制剂

Flavopiridol（Alvocidib）是一种细胞周期蛋白依赖性激酶抑制剂，与ATP竞争性抑制CDK，包括CDK1， CDK2， CDK4和CDK6，CDK9。作用于CDK1， 2， 4， 6，9比作用于CDK7更具有选择性，用于治疗慢性淋巴细胞性白血病。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Zhiyuan Zhao, .et al. CDK9 and SPT5 proteins are specifically required for expression of herpes simplex virus 1 replication-dependent late genes, J Biol Chem, 2017, Sep 15; 292(37): 15489-15500 PMID: 28743741
- Sami Kukkonen, .et al. HIV-1 Tat second exon limits the extent of Tat-mediated modulation of interferon-stimulated genes in antigen presenting cells, Retrovirology., 2014, 11: 30. PMID: 24742347
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BKM120 (NVP-BKM120, Buparlisib)

Catalog No. A11016
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PI3K 抑制剂?

BKM120 (NVP-BKM120,Buparlisib)是生物可利用的口服泛I类磷脂酰肌醇3激酶（PI3K）激酶抑制剂，在无细胞试验中作用于p110α/β/δ/γ的。对VPS34，mTOR，DNAPK的作用效果下降，而对 PI4Kβ几乎没有活性。了解更多

Product Citations (11)

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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Takaaki Fujimura, .et al. Enhanced antitumor effect of alectinib in combination with cyclin-dependent kinase 4/6 inhibitor against RET-fusion-positive non-small cell lung cancer cells, Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
- Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Saijo A, .et al. Bone marrow-derived fibrocytes promote stem cell-like properties of lung cancer cells, Cancer Lett, 2018, May 1;421:17-27 PMID: 29448000
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rogers HA, .et al. PI3K pathway activation provides a novel therapeutic target for pediatric ependymoma and is an independent marker of progression-free survival., Clin Cancer Res., 2013, Dec 1;19(23):6450-60 PMID: 24077346
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PLX4032 (Vemurafenib)

Catalog No. A10739
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Raf 抑制剂

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。了解更多

Product Citations (11)

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- Lee YJ, .et al. Overexpression of Dock180 and Elmo1 in melanoma is associated with cell survival and migration, Research Square, 2022, April 27th
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
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GDC-0941 (Pictilisib)

Catalog No. A10421
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PI3K 抑制剂

GDC-0941 (Pictilisib)是一种强效、选择性、口服生物可利用的I类PI3激酶(PI3K)抑制剂，p110 α、β、δ和γ亚型、DNA-PK和mTOR的IC50值分别为3、33、3、75、1230和580 nM。了解更多

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- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
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CHIR-99021

Catalog No. A10199
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GSK-3 抑制剂

CHIR99021是一种GSK-3α和GSK-3β抑制剂，IC50值分别为10和6.7 nM。了解更多

Product Citations (6)

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- Adam Pietrobon, .et al. Renal organoid modeling of tuberous sclerosis complex reveals lesion features arise from diverse developmental processes, Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Takayuki Miyoshi, .et al. Successful induction of human chemically induced liver progenitors with small molecules from damaged liver, J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Tomoki Kamatani, .et al. Evaluation of immunosuppression protocols for MHC-matched allogeneic iPS cell-based transplantation using a mouse skin transplantation model, Inflamm Regen, 2022, Feb 2;42(1):4 PMID: 35105370
- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Otsuka R, .et al. Efficient generation of thymic epithelium from induced pluripotent stem cells that prolongs allograft survival, Sci Rep, 2020, Jan 14;10(1):224 PMID: 31937817
- Yu Huang, .et al. Development of Bifunctional Three-Dimensional Cysts from Chemically Induced Liver Progenitors, Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
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Saracatinib (AZD0530)

Catalog No. A10108
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Src/Abl 抑制剂

Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。了解更多

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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TAK-875 (Fasiglifam)

Catalog No. A11018
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GPR 激动剂

TAK-875 (Fasiglifam)是一种有效的，选择性的GPR40激动剂。了解更多

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- Ying Liu, .et al. A synthetic free fatty acid-regulated transgene switch in mammalian cells and mice, Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. Mechanistic insights into the detection of free fatty and bile acids by ileal glucagon-like peptide-1 secreting cells, Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. Potentiation of Glucose-stimulated Insulin Secretion by the GPR40-PLC-TRPC Pathway in Pancreatic β-Cells, Sci Rep, 2016, 6: 25912 PMID: 27180622
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CHR2797 (Tosedostat)

Catalog No. A10208
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Aminopeptidase 抑制剂

CHR2797 (Tosedostat)是一种新型金属酶抑制剂，在体内和体外对多种肿瘤细胞系均具有抗增殖作用，并表现出选择性。了解更多

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AZD6482

Catalog No. A10112
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PI3K 抑制剂

AZD6482是一种PI3Kβ抑制剂，(IC50 = 0.021M)。了解更多

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Masitinib ( AB1010)

Catalog No. A10558
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c-Kit 抑制剂

Masitinib (AB1010)是一种蛋白质酪氨酸激酶抑制剂。了解更多

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- S Masson ,etc. Inhibition of Cell Signalling in Neoplastic Canine Mast Cells. , 2014, .
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Canertinib (CI-1033)

Catalog No. A10211
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HER2/ErbB2 抑制剂

Canertinib (CI-1033)是一种不可逆的酪氨酸激酶抑制剂，对EGFR（IC50 0.8 nM），HER-2（IC50 19 nM）和ErbB-4（IC50 7 nM）具有活性。了解更多

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- Fukuda N, .et al. Rapid Evaluation of Tyrosine Kinase Activity of Membrane Integrated Human Epidermal Growth Factor Receptor Using the Yeast Gγ Recruitment System, ACS Synth Biol., 2015, 4(4):421-9 PMID: 25006755
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R406 besylate

Catalog No. A10769
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Syk 抑制剂

R406 besylate是一种口服酪氨酸激酶抑制剂，IC50为41 nM。对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。了解更多

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- Gabriella Leung, .et al. ARPC1B binds WASP to control actin polymerization and curtail tonic signaling in B cells, JCI insight, 2021, Dec 8;6(23):e149376 PMID: 34673575

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