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Marbofloxacin

Catalog No. A10557
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Topoisomerase 抑制剂

Marbofloxacin是有效的第三代氟喹诺酮类抗生素，通过抑制细菌DNA复制起作用。了解更多

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Raltitrexed (Tomudex)

Catalog No. A10776
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DNA/RNA Synthesis 抑制剂

Raltitrexed (Tomudex)是胸苷酸合酶的抑制剂，也是使用中最强的抗代谢物之一。了解更多

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- Yool Lee, .et al. Time-of-day specificity of anticancer drugs may be mediated by circadian regulation of the cell cycle, Sci Adv, 2021, 7
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Topotecan HCl (Hycamtin)

Catalog No. A10939
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DNA topoisomerase I 抑制剂

Topotecan HCl (Hycamtin)是一种化学治疗剂，是拓扑异构酶抑制剂。了解更多

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Vatalanib (PTK787) 2HCl

Catalog No. A10967
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VEGFR 抑制剂

Vatalanib (PTK787) 2HCl是一种小分子蛋白激酶抑制剂，可抑制抑制所有已知VEGF受体以及血小板衍生的生长因子受体β和c-kit的血管生成，但对VEGFR-2的选择性最高。了解更多

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Abiraterone (CB-7598)

Catalog No. A10020
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CYP17 抑制剂

Abiraterone (CB-7598)是一种有效CYP17抑制剂，20裂合酶（CYP17A1）。了解更多

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Abiraterone Acetate (CB7630)

Catalog No. A11058
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CYP17 抑制剂

Abiraterone Acetate是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂。了解更多

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Docetaxel (Taxotere)

Catalog No. A10326
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Microtubule Associated 抑制剂

Docetaxel (Taxotere)多西他赛一种taxol类似物，是一种microtubules解聚抑制剂，通过结合于稳定的微管发挥作用。了解更多

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Paclitaxel (Taxol)

Catalog No. A10689
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Microtubule Associated 抑制剂

Paclitaxel (Taxol)是一种有丝分裂抑制剂，可稳定微管，从而干扰细胞分裂过程中微管的正常分解，在人内皮细胞中IC50为0.1pM。了解更多

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- Yu Pan, .et al. The nature of the modification at position 37 of tRNAPhe correlates with acquired taxol resistance, Nucleic Acids Res, 2021, Jan 11;49(1):38-52 PMID: 33290562
- Li-Li Li, .et al. Resonance energy transfer sensitises and monitors in situ switching of LOV2-based optogenetic actuators, Nat Commun, 2020, Oct 9;11(1):5107 PMID: 33037199
- Baglo Y, .et al. Harnessing the Potential Synergistic Interplay Between Photosensitizer Dark Toxicity and Chemotherapy, Photochem Photobiol, 2019, Dec 19 PMID: 31856423
- Owiti AO, .et al. PSMA Antibody-Conjugated Pentablock Copolymer Nanomicellar Formulation for Targeted Delivery to Prostate Cancer, AAPS PharmSciTech, 2018, Nov;19(8):3534-3549 PMID: 30151731
- Owiti AO, .et al. Strategic Pentablock Copolymer Nanomicellar Formulation for Paclitaxel Delivery System, AAPS PharmSciTech, 2018, Oct;19(7):3110-3122 PMID: 30112614
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Vincristine sulfate

Catalog No. A10973
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Tubulin 抑制剂

Vincristine sulfate是一种有丝分裂抑制剂。了解更多

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Epothilone B (EPO906)

Catalog No. A10360
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Microtubule Associated 抑制剂

Epothilone B (EPO906)是一种紫杉醇样microtubule稳定剂。了解更多

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- Yicheng Zhu, .et al. Combinatrial treatment of anti-High Mobility Group Box-1 monoclonal antibody and epothilone B improves functional recovery after spinal cord contusion injury, Neurosci Res, 2021, Apr 17 PMID: 33864880
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Dasatinib (BMS-354825)

Catalog No. A10290
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Abl-Src 抑制剂

Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。了解更多

Product Citations (10)

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- Chihiro Motozono, .et al. The SARS-CoV-2 Omicron BA.1 spike G446S mutation potentiates antiviral T-cell recognition, Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- 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
- David E J Klawon, .et al. Altered selection on a single self-ligand promotes susceptibility to organ-specific T cell infiltration, J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- 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
- 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
- Sano T, .et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- 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
- John D. Leonard, .et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- 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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BMS-754807

Catalog No. A11059
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IGF-1R 抑制剂

BMS-754807是一种有效的，口服活性生长因子1受体/胰岛素受体家族靶向的激酶抑制剂。了解更多

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- 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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CX-4945 (Silmitasertib)

Catalog No. A11060
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CK2 抑制剂

CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，可抑制人脐静脉内皮细胞迁移，管形成，并阻止癌细胞中CK2依赖性缺氧诱导的因子1α（HIF-1α）转录。了解更多

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- Xixi Zhao, .et al. Phosphorylation and Stabilization of PD-L1 by CK2 Suppresses Dendritic Cell Function, Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. CX-4945 and siRNA-Mediated Knockdown of CK2 Improves Cisplatin Response in HPV(+) and HPV(-) HNSCC Cell Lines, Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. PRMT6 methylation of RCC1 regulates mitosis, tumorigenicity, and radiation response of glioblastoma stem cells, Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. Protein kinase CK2 impact on intracellular calcium homeostasis in prostate cancer, Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. Protein kinase CK2 is involved in zinc homeostasis in breast and prostate cancer cells, Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. Human Rad17?C-terminal tail is phosphorylated by concerted action of CK1δ/ε and CK2 to promote interaction with the 9-1-1 complex, Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. Casein kinase 2 promotes interaction between Rad17 and the 9-1-1 complex through constitutive phosphorylation of the C-terminal tail of human Rad17, Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. Casein kinase 2 controls the survival of normal thymic and leukemic γδ T cells via promotion of AKT signaling, Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. mTORC1 and CK2 coordinate ternary and eIF4F complex assembly, Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. Protein Kinase CK2 Regulates Leukocyte-Endothelial Cell Interactions during Ischemia and Reperfusion in Striated Skin Muscle, Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. Role of protein kinase CK2 in the dynamic interaction of platelets, leukocytes and endothelial cells during thrombus formation., Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. Inhibition of protein kinase CK2 suppresses tumor necrosis factor (TNF)-α-induced leukocyte-endothelial cell interaction., Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. Adult B-cell acute lymphoblastic leukemia cells display decreased PTEN activity and constitutive hyperactivation of PI3K/Akt pathway despite high PTEN protein levels, Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
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ENMD-2076

Catalog No. A10352
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Aurora A / FLT3 抑制剂

ENMD-2076具有针对Aurora A和Flt3的选择性活性，IC50为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对VEGFR2/KDR和VEGFR3，FGFR1和FGFR2和PDGFRα的作用较小。阶段2。了解更多

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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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Curcumol

Catalog No. A10247
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JAK2 抑制剂

Curcumol是常见的传统中药，具有抗肿瘤活性。了解更多

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Taxifolin

Catalog No. A10893
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VEGFR-2 抑制剂

Taxifolin以很大的结合能值结合在VEGFR-2激酶的ATP结合位点上，并起I型竞争性抑制剂的作用。了解更多

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- Keji Yu, .et al. A role for ascorbate conjugates of (+)-catechin in proanthocyanidin polymerization, Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. Antidiabetic Effect of Taxifolin in Cultured L6 Myotubes and Type 2 Diabetic Model KK-Ay/Ta Mice with Hyperglycemia and Hyperuricemia, Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. Anti-hyperuricemic effect of taxifolin in cultured hepatocytes and model mice, Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
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GSK461364

Catalog No. A10442
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PLK 抑制剂

GSK461364 是polo样激酶1 (Plk1)的ATP竞争性抑制剂。了解更多

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SB 216763

Catalog No. A10825
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GSK-3 抑制剂

SB 216763是一种有效且具有选择性的细胞渗透性ATP竞争性GSK3α抑制剂，IC50值为34 nM（与GSK3β相似的效力）。了解更多

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SB 415286

Catalog No. A11061
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GSK-3 抑制剂

SB 415286是一种有效且具有选择性的细胞渗透性ATP竞争性GSK3α抑制剂，IC50值为78 nM（与GSK3β相似的效价），Ki值为31 nM。了解更多

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CX-5461

Catalog No. A11065
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DNA/RNA Synthesis 抑制剂

CX-5461是RNA聚合酶I（Pol I）的一流的非遗传毒性小分子靶向抑制剂，可激活p53途径而不会引起DNA损伤。了解更多

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- Taro Mannena, .et al. Distinct RNA polymerase transcripts direct the assembly of phase-separated DBC1 nuclear bodies in different cell lines, Mol Biol Cell, 2021, 32:ar33, 1?C11 PMID: 34495685
- Shuichiro Okamoto, .et al. The rRNA synthesis inhibitor CX-5461 may induce autophagy that inhibits anticancer drug-induced cell damage to leukemia cells, Biosci Biotechnol Biochem, 2020, Aug 15;1-8 PMID: 32799625
- Ahmed Abdullah Ahmed, .et al. A G-quadruplex-binding compound shows potent activity in human gemcitabine-resistant pancreatic cancer cells, Sci Rep, 2020, 10: 12192 PMID: 32699225
- Abed Saady, .et al. Applying styryl quinolinium fluorescent probes for imaging of ribosomal RNA in living cells, Dyes Pigm, 2020, 174: 107986
- Jackobel AJ, .et al. DNA binding preferences of S. cerevisiae RNA polymerase I Core Factor reveal a preference for the GC-minor groove and a conserved binding mechanism, Biochim Biophys Acta Gene Regul Mech, 2019, Aug 2:194408 PMID: 31382053
- Hiroaki Suzuki, .et al. The proline-arginine repeat protein linked to C9-ALS/FTD causes neuronal toxicity by inhibiting the DEAD-box RNA helicase-mediated ribosome biogenesi, Cell Death Dis, 2018, Oct; 9(10): 975 PMID: 30250194
- Anastasia Gelgor, .et al. Nucleolar stress enhances lytic reactivation of the Kaposi??s sarcoma-associated herpesvirus, Oncotarget, 2018, Mar 2; 9(17): 13822-13833 PMID: 29568397
- Wang ZF, .et al. The Hairpin Form of r(G4C2)exp in c9ALS/FTD Is Repeat-Associated Non-ATG Translated and a Target for Bioactive Small Molecules, Cell Chem Biol, 2018, Nov 29. pii: S2451-9456(18)30378-7 PMID: 30503283
- Yuko Fujiwara, .et al. A Nucleolar Stress-Specific p53-miR-101 Molecular Circuit Functions as an Intrinsic Tumor-Suppressor Network, EBioMedicine, 2018, Jul; 33: 33-48 PMID: 30049386
- Maïmouna Coura Kone, .et al. Three-Dimensional Distribution of UBF and Nopp140 in Relationship to Ribosomal DNA Transcription During Mouse Preimplantation Development, Biol Reprod, 2016, Apr;94(4):95, 1-12 PMID: 26984997
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TAK-901

Catalog No. A11067
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Aurora Kinase A/B 抑制剂

TAK-901是一种新型Aurora A/B抑制剂，IC50为21 nM/15 nM。它不是细胞JAK2，c-Src或Abl的有效抑制剂。了解更多

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S/GSK1349572 (Dolutegravir)

Catalog No. A11068
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HIV integrase 抑制剂

S/GSK1349572是有效的下一代HIV整合酶抑制剂，并通过60个整合酶突变分子克隆证实了优异的耐药性。了解更多

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- Lea El Khoury, .et al. Spectrometric and computational studies of the binding of HIV-1 integrase inhibitors to viral DNA extremities, PeerJ Preprints, 2019, 7:e27833v1
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MK-0752

Catalog No. A11194
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Gamma-secretase 抑制剂

MK-0752抑制Notch信号通路，这可能会导致Notch信号通路被过度激活的肿瘤细胞诱导生长停滞和凋亡。了解更多

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PF-562271

Catalog No. A11192
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FAK 抑制剂

PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。了解更多

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- Jiping Yue, .et al. In vivo epidermal migration requires focal adhesion targeting of ACF7, Nat Commun, 2016, 7: 11692 PMID: 27216888
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GSK1904529A

Catalog No. A10440
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IGF-1R 抑制剂

GSK1904529A分别用27和25 nmol/L的IC(50)s选择性抑制IGF-IR和IR。了解更多

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AZD4547

Catalog No. A11075
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FGFR 抑制剂

AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。了解更多

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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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ZM 336372

Catalog No. A11077
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C-Raf 抑制剂

ZM 336372是有效的ATP Raf-1体外竞争性抑制剂 (IC50 = 70 nM)。了解更多

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PKI-587 ( Gedatolisib )

Catalog No. A11079
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PI3K/mTOR 抑制剂

PKI-587 (Gedatolisib)是一种高效的PI3K/mTOR激酶抑制剂，可抑制PI3K-α，β，γ，δ亚型和mTOR，IC50分别为0.4、6.0、5.4、6.0和1.6 nM。了解更多

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TG-101348 (Fedratinib, SAR302503)

Catalog No. A11082
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JAK2/FLT3 抑制剂

TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型，ATP竞争性和选择性抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。了解更多

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GW788388

Catalog No. A11083
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TGF-beta/Smad 抑制剂

GW788388是有效的，口服活性的，选择性的转化生长因子β受体I（TGF-βR1）（激活素受体样激酶5，ALK5）抑制剂,无细胞试验中IC50为18 nM，也抑制TGF-βII型受体和activin II型受体活性，但不抑制BMP II型受体。了解更多

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Telaprevir (VX-950)

Catalog No. A10902
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HCV NS3-4A protease 抑制剂

Telaprevir (VX-950)被称为蛋白酶抑制剂，可抑制丙型肝炎病毒NS3.4A丝氨酸蛋白酶。了解更多

Product Citations (9)

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- Mahim Khan, .et al. Hesperidin identified from Citrus extracts potently inhibits HCV genotype 3a NS3 protease, BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Adita Ayu Permanasari, .et al. An in vitro study of an Artocarpus heterophyllus substance as a hepatitis C antiviral and its combination with current anti-HCV drugs, BMC Complement Med Ther, 2021, Oct 12;21(1):260 PMID: 34641875
- Che C Colpitts, .et al. Hepatitis C virus exploits cyclophilin A to evade PKR, eLife, 2020, 9: e52237 PMID: 32539931
- TS Wahyuni, .et al. Enhancement of Anti-Hepatitis C Virus Activity by the Combination of Chalepin From Ruta Angustifolia and Current Antiviral Drugs, Southeast Asian J Trop Med public health, 2020, 51(1)
- Stefan Bittmann, .et al. TMPRSS2-Inhibitors Play a role in Cell Entry Mechanism of COVID-19: An Insight into Camostat and Nafamostat, J Regen Biol Med, 2020, 2(2):1-3
- Wahyuni TS, .et al. Synergistic anti-hepatitis C virus activity of Ruta angustifolia extract with NS3 protein inhibitor, J Basic Clin Physiol Pharmacol, 2019, Dec 14 PMID: 31837259
- Jacobs CL, .et al. StaPLs: versatile genetically encoded modules for engineering drug-inducible proteins, Nat Methods, 2018, Jul;15(7):523-526 PMID: 29967496
- Apriyanto DR, .et al. Anti-Hepatitis C Virus Activity of a Crude Extract from Longan (Dimocarpus longan Lour.) Leaves, Jpn J Infect Dis, 2016, May 20;69(3):213-20 PMID: 26255732
- Mizuki Yamamoto, .et al. Identification of Nafamostat as a Potent Inhibitor of Middle East Respiratory Syndrome Coronavirus S Protein-Mediated Membrane Fusion Using the Split-Protein-Based Cell-Cell Fusion Assay, Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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BIBR-1048 (Dabigatran etexilate)

Catalog No. A10139
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Thrombin 抑制剂

BIBR-1048 (Dabigatran etexilate)是dabigatran的前体药物，dabigatran是一种有效的、非肽类小分子化合物，可特异地、可逆性地抑制游离的和结合了血凝块的凝血酶。了解更多

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Anacetrapib (MK-0859)

Catalog No. A11084
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CETP 抑制剂

Anacetrapib (MK-0859)是一种有效的，选择性，可逆的rhCETP和突变CETP(C13S)抑制剂，IC50分别为7.9 nM和11.8 nM，提高HDL-C，降低LDL-C，不提高醛固酮和血压。了解更多

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LY315920 (Varespladib)

Catalog No. A10548
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HnsPLA 抑制剂

LY315920 (Varespladib)是分泌型磷脂酶A2 (sPLA2)的IIa、V和X亚型的抑制剂。了解更多

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- Yap WH, .et al. Differential effects of sPLA2-GV and GX on cellular proliferation and lipid accumulation in HT29 colon cancer cells, Mol Cell Biochem, 2018, Oct;447(1-2):93-101 PMID: 29374817
- Yamato Okita, .et al. Interleukin-22-Induced Antimicrobial Phospholipase A2 Group IIA Mediates Protective Innate Immunity of Nonhematopoietic Cells against Listeria monocytogenes, Infect Immun, 2016, Feb; 84(2): 573-579 PMID: 26644377
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CHIR-98014

Catalog No. A11085
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GSK-3 抑制剂

CHIR-98014是一种非常有效的，选择性的，细胞可渗透的GSK-3抑制剂。了解更多

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ARQ 197 (Tivantinib)

Catalog No. A11087
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c-Met 抑制剂

ARQ-197是c-Met受体酪氨酸激酶的选择性抑制剂, 在无细胞试验中Ki为0.355 μM，对Ron几乎没有作用活性，对EGFR， InsR， PDGFRα和FGFR1/4没有抑制作用。了解更多

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- Wang L, .et al. Bispecific Aptamer Induced Artificial Protein-Pairing: A Strategy for Selective Inhibition of Receptor Function, J Am Chem Soc, 2019, Aug 14;141(32):12673-12681 PMID: 31381313
- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
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Pyroxamide (NSC 696085)

Catalog No. A10764
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HDAC 抑制剂

Pyroxamide (NSC 696085)是亲和纯化的HDAC1的有效抑制剂，可导致乙酰化核心组蛋白在用该试剂培养的MEL细胞中积累。了解更多

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Nitisinone

Catalog No. A11093
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HPPD 抑制剂

Nitrisinone是一种竞争性抑制剂，可逆地抑制4-羟基苯基丙酮酸氧化酶（双加氧酶）。了解更多

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DAPT (GSI-IX)

Catalog No. A10288
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Gamma secretase 抑制剂

DAPT (GSI-IX)是一种γ-分泌酶抑制剂，可导致人原代神经元培养物中Aβ40和Aβ42水平降低，总Aβ和Aβ42的IC50值分别为115和200 nM。了解更多

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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture, Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
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Dapagliflozin (BMS512148)

Catalog No. A10285
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SGLT2 抑制剂

Dapagliflozin (BMS512148)抑制钠-葡萄糖转运蛋白（SGLT2）的亚型2，后者负责肾脏中至少90％的葡萄糖重吸收。了解更多

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- David Papadopoli, .et al. Perturbations of cancer cell metabolism by the antidiabetic drug canagliflozin, Neoplasia, 2021, Apr;23(4):391-399 PMID: 33784591
- Neil Tanday, .et al. Dapagliflozin exerts positive effects on beta cells, decreases glucagon and does not alter beta- to alpha-cell transdifferentiation in mouse models of diabetes and insulin resistance, Biochem Pharmacol, 2020, Jul;177:114009 PMID: 32360307
- Subramaniam M, .et al. Comparison of Intestinal Glucose Flux and Electrogenic Current Demonstrates Two Absorptive Pathways in Pig and One in Nile Tilapia and Rainbow Trout, Am J Physiol Regul Integr Comp Physiol, 2019, Nov 20 PMID: 31746628
- Marina Subramaniam, .et al. Sigmoidal kinetics define porcine intestinal segregation of electrogenic monosaccharide transport systems as having multiple transporter population involvement, Physiol Rep, 2019, May; 7(9): e14090 PMID: 31062524
- Angelopoulou A, .et al. Magnetic Nanoparticles for the Delivery of Dapagliflozin to Hypoxic Tumors: Physicochemical Characterization and Cell Studies, AAPS PharmSciTech, 2018, Feb;19(2):621-633 PMID: 8924948
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NU-7441 (KU-57788)

Catalog No. A11098
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DNA-PK 抑制剂

NU-7441 (KU-57788)是一种有效的选择性DNA依赖性蛋白激酶（DNA-PK）抑制剂。对于DNA-PK，mTOR，PI 3-K，ATM和ATR，IC50值分别为14、1700、5000，> 100000和> 100000 nM。了解更多

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- Shahar Biechonski, .et al. Attenuated DNA damage responses and increased apoptosis characterize human hematopoietic stem cells exposed to irradiation, Sci Rep, 2018, Apr 17 PMID: 29666389
- Ihara M, .et al. Expression of the DNA-dependent protein kinase catalytic subunit is associated with the radiosensitivity of human thyroid cancer cell lines, J Radiat Res, 2018, Nov 23 PMID: 30476230
- Chwastek J, .et al. The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a γH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D, Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
- Masaaki Yanai, .et al. DNA-PK Inhibition by NU7441 Enhances Chemosensitivity to Topoisomerase Inhibitor in Non-Small Cell Lung Carcinoma Cells by Blocking DNA Damage Repair, Yonago Acta Med, 2017, Mar; 60(1): 9-15 PMID: 28331416
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AS-252424

Catalog No. A11099
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PI3K 抑制剂

AS-252424是有效的PI3K抑制剂，对γ亚型具有选择性。它抑制人重组PI3Kγ，α，β和δ，IC50值分别为30、940、20,000和20,000 nM。了解更多

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Canagliflozin

Catalog No. A11100
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SGLT2 抑制剂

canagliflozin是2型亚钠葡萄糖转运蛋白（SGLT2）的抑制剂,作用于hSGLT2，无细胞试验中IC50为2.2 nM，比作用于hSGLT1选择性高413倍。了解更多

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- David Papadopoli, .et al. Perturbations of cancer cell metabolism by the antidiabetic drug canagliflozin, Neoplasia, 2021, Apr;23(4):391-399 PMID: 33784591
- Angelopoulou A, .et al. Canagliflozin-loaded magnetic nanoparticles as potential treatment of hypoxic tumors in combination with radiotherapy, Nanomedicine, 2018, Oct;13(19):2435-2454 PMID: 30311542
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AZ-960

Catalog No. A10104
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JAK2抑制剂

AZ-960是一种有效的，选择性的和ATP竞争性的JAK2抑制剂，在体外抑制JAK2激酶的Ki为0.45 nM，并诱导成年T细胞白血病（ATL）细胞的生长停滞和凋亡了解更多

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Methotrexate (Abitrexate)

Catalog No. A10021
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DHFR 抑制剂

Methotrexate (Abitrexate)是一种抑制胸苷酸合成酶和从头嘌呤合成的细胞毒剂。了解更多

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Saxagliptin (BMS-477118)

Catalog No. A11109
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DPP-4 抑制剂

Saxagliptin (BMS-477118)是一种新型二肽基肽酶4（DPP-4）抑制剂，IC50为50 nM。了解更多

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- OHE El-Shoubashy, .et al. Comparative study of HPLC-DAD and HPTLC for the simultaneous determination of a new multitarget antidiabetic ternary mixture in combined tablets, JPC, 2020, 33, 59-70
- Sato T, .et al. DPP8 is a novel therapeutic target for multiple myeloma, Sci Rep, 2019, Dec 2;9(1):18094 PMID: 31792328
- Chintan N. Koyani, .et al. Saxagliptin but Not Sitagliptin Inhibits CaMKII and PKC via DPP9 Inhibition in Cardiomyocytes, Front Physiol, 2018, 9: 1622 PMID: 30487758
- Koyani CN, .et al. Dipeptidyl peptidase-4 independent cardiac dysfunction links saxagliptin to heart failure, Biochem Pharmacol, 2016, Dec 1;145:64-80 PMID: 28859968
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Rasagiline

Catalog No. A11111
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MAO B 抑制剂

Rasagiline是MAO-B（单胺氧化酶-B）的选择性不可逆抑制剂。了解更多

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Avasimibe (CI-1011)

Catalog No. A10102
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CYP17 抑制剂

Avasimibe (CI-1011)是口服可生物利用的酰基辅酶A：胆固醇O-酰基转移酶（ACAT）抑制剂，IC50分别为2.9 μM， 13.9 μM和26.5 μM。了解更多

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- Yuyan Zhu, .et al. Pharmacological inhibition of acyl-coenzyme A:cholesterol acyltransferase alleviates obesity and insulin resistance in diet-induced obese mice by regulating food intake, Metabolism, 2021, Oct;123:154861 PMID: 34371065
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TOK-001 (Galeterone)

Catalog No. A11138
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CYP17 抑制剂

TOK-001 (Galeterone)既是雄激素受体拮抗剂又是CYP17A1抑制剂。了解更多

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