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Fexofenadine HCl

Catalog No. A11859
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COX 抑制剂/histamine H1 receptor 激动剂

Fexofenadine Hydrochloride是一种抗组胺药，可抑制Cox-1，Cox-2，并且是组胺H1受体激动剂，IC50为246 nM。了解更多

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Darunavir Ethanolate (Prezista)

Catalog No. A11853
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HIV protease 抑制剂

Darunavir Ethanolate (Prezista)是一种HIV蛋白酶抑制剂。了解更多

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Tideglusib

Catalog No. A11592
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GSK-3 抑制剂

Tideglusib是一种不可逆的，非ATP竞争性的GSK-3β抑制剂，无细胞试验中IC50为60 nM。用于治疗阿尔茨海默氏病和进行性核上性麻痹。了解更多

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PFI-1

Catalog No. A12545
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BET 抑制剂

PFI-1是BET溴结构域抑制剂，对BRD2和BRD4表现出抑制活性。了解更多

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NSC 23766

Catalog No. A12546
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Rac1 activation 抑制剂

SC 23766是Rac1-GEF相互作用的选择性抑制剂。通过Rac特异性鸟嘌呤核苷酸交换因子（GEF）TrioN和Tiam1（IC50为50 μM）阻止Rac1激活，而不影响Cdc42或RhoA激活。了解更多

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Ixabepilone

Catalog No. A11449
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microtubule 抑制剂

Ixabepilone是epothilone B类似物。了解更多

Product Citations (3)

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- Dong-Sheng Cao, .et al. A Multi-Scale Systems Pharmacology Approach Uncovers the Anti-Cancer Molecular Mechanism of Ixabepilone, Eur J Med Chem, 2020, Aug 1;199:112421 PMID: 32428794
- Hoque M, .et al. Changes in cell morphology guide identification of tubulin as the off-target for protein kinase inhibitors, Pharmacol Res, 2018, Aug;134:166-178 PMID: 29944980
- APRIL L. RISINGER, .et al. Breast Cancer Cell Lines Exhibit Differential Sensitivities to Microtubule-targeting Drugs Independent of Doubling Time, Anticancer Res, 2015, Nov; 35(11): 5845-5850. PMID: 26504006
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XL-888

Catalog No. A11251
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HSP90 抑制剂

XL888是口服可生物利用的，具有ATP竞争性的小分子热休克蛋白90（Hsp90）抑制剂，IC50为24 nM。具有潜在的抗肿瘤活性。了解更多

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GSK-923295

Catalog No. A11435
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CENP-E 抑制剂

GSK-923295是有丝分裂驱动蛋白着丝粒相关蛋白E（CENP-E）的小分子抑制剂。了解更多

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Etomoxir (sodium salt)

Catalog No. A11415
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CPT-1 irreversible 抑制剂

Etomoxir (sodium salt)是肉碱棕榈酰转移酶A(CPT1)的抑制剂，它是长链酰基辅酶A酯氧化所必需的。也是线粒体CPT1的强抑制剂和抗糖尿病药物的候选药物。了解更多

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- A. Geneste, .et al. Adipocyte-conditioned medium induces resistance of breast cancer cells to lapatinib, BMC Pharmacol Toxicol, 2020, 21: 61 PMID: 32795383
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Dapivirine

Catalog No. A12587
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HIV reverse transcriptase 抑制剂

Dapivirine是一种有效的非核苷逆转录酶抑制剂（NNRTI）。了解更多

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MSX-122

Catalog No. A12596
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CXCR4 抑制剂

MSX-122是口服可生物利用的CXCR4抑制剂（IC50 =?10 nM），具有潜在的抗肿瘤和抗病毒活性。CXCR4抑制剂MSX-122与趋化因子受体CXCR4结合，阻止基质衍生因子-1（SDF-1）与CXCR4受体和受体激活结合，这可能导致肿瘤细胞增殖和迁移减少。了解更多

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TAK-715

Catalog No. A11582
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p38 MAPK 抑制剂

TAK 715是p38 MAPK抑制剂（p38MAPKα的IC50 = 7.1 nM），Wnt /β-catenin信号传导抑制剂，并抑制22种激酶（包括CK1δ/ε）超过80％。了解更多

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- Dongdong Fang, etc. Epithelial-Mesenchymal Transition of Ovarian Cancer Cells Is Sustained by Rac1 through Simultaneous Activation of MEK1/2 and Src Signaling Pathways. Oncogene. 2017 Mar; 36(11): 1546–1558.
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Tariquidar (XR9576)

Catalog No. A11584
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P-gp 抑制剂

Tariquidar (XR9576)是一种P-糖蛋白药物外排泵抑制剂。了解更多

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- Yuko Sasaki, .et al. Intestinal Permeability of Drugs in Caco-2 Cells Cultured in Microfluidic Devices, Biol Pharm Bull, 2022, 45(9):1246-1253 PMID: 36047192
- Sugisawa N, .et al. Novel Potent ABCB1 Modulator, Phenethylisoquinoline Alkaloid, Reverses Multidrug Resistance in Cancer Cell, Mol Pharm, 2018, Sep 4;15(9):4021-4030 PMID: 30052463
- Samy A. F. Morad, .et al. Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer, Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Debora Petroni, .et al. Synthesis and In Vivo Imaging of N-(3-[11C]Methoxybenzyl)-2-(3-Methoxyphenyl)ethylaniline as a Potential Targeting Agent for P-glycoprotein, Mol Imaging Biol, 2016, Dec;18(6):916-923 PMID: 27234445
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Torin 1

Catalog No. A11587
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mTOR 抑制剂

Torin1是mTOR的有效抑制剂，IC50为2-10 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
- Kowalsky AH, .et al. The GATOR2?CmTORC2 axis mediates Sestrin2-induced AKT Ser/Thr kinase activation, J Biol Chem, 2020, Feb 14;295(7):1769-1780 PMID: 31915252
- Ashyad Rayhan, .et al. Using genetic buffering relationships identified in fission yeast to reveal susceptibilities in cells lacking hamartin or tuberin function, Biol Open, 2018, Jan 15; 7(1): bio031302 PMID: 29343513
- 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
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T-705 (Favipiravir)

Catalog No. A11590
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viral RNA polymerase 抑制剂

T-705 (Favipiravir)是一种有效的选择性RNA-dependent RNA polymerase抑制剂，在体外和体内均表现出有效的抗流感病毒活性。了解更多

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- Satoko Yamaoka, .et al. Development of accelerated high-throughput antiviral screening systems for emerging orthomyxoviruses, Antiviral Res, 2022, Apr;200:105291 PMID: 35296419
- Crystal A Mendoza, .et al. The NF- κB inhibitor, SC75741, is a novel antiviral against emerging tick-borne bandaviruses, Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
- Liva Checkmahomed, .et al. In Vitro Combinations of Baloxavir Acid and Other Inhibitors against Seasonal Influenza A Viruses, Viruses, 2020, Oct; 12(10): 1139 PMID: 33049959
- JE Comer, .et al. Filovirus Virulence in Interferon α,β and γ Double Knockout Mice, and Treatment with Favipiravir, Viruses, 2019, Feb 3;11(2). pii: E137 PMID: 30717492
- Ma J, .et al. Enhancing the antiviral potency of ER α-glucosidase inhibitor IHVR-19029 against hemorrhagic fever viruses in vitro and in vivo, Antiviral Res, 2018, Feb;150:112-122 PMID: 29253498
- Ji-Ae Kim, .et al. Favipiravir and Ribavirin Inhibit Replication of Asian and African Strains of Zika Virus in Different Cell Models, Viruses, 2018, Feb; 10(2): 72 PMID: 29425176
- Haejin Chun, .et al. Efficient antiviral co-delivery using polymersomes by controlling the surface density of cell-targeting groups for influenza A virus treatment, Polym Chem, 2018, 9: 2116-2123
- Baz M, .et al. Combination Therapy with Oseltamivir and Favipiravir Delays Mortality but Does Not Prevent Oseltamivir Resistance in Immunodeficient Mice Infected with Pandemic A(H1N1) Influenza Virus, Viruses, 2018, Nov 3;10(11) PMID: 30400276
- Sehee Park, .et al. Combination Effects of Peramivir and Favipiravir against Oseltamivir-Resistant 2009 Pandemic Influenza A(H1N1) Infection in Mice, PLoS One., 2014, 9(7): e101325 PMID: 24992479
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GSK 525762A (I-BET-762)

Catalog No. A11440
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BET 抑制剂

GSK 525762A (I-BET-762)是BET(溴域和末端外)家族的小分子抑制剂。了解更多

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PJ 34 hydrochloride

Catalog No. A12665
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PARP 抑制剂

PJ 34 hydrochloride是聚（ADP-核糖）聚合酶（PARP）（EC50 = 20 nM）的有效抑制剂。了解更多

Product Citations (2)

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- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
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ONX-0914

Catalog No. A12653
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Immunoproteasome 抑制剂

ONX 0914是有效，选择性的免疫蛋白酶体亚基LMP7的抑制剂，在自身免疫性疾病（如类风湿性关节炎，炎性肠病和狼疮）中具有潜在的治疗应用。ONX 0914被设计为一种有效的免疫蛋白酶抑制剂，对组成型蛋白酶体的交叉反应最小。了解更多

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- Yuki Sasaki, .et al. Blockade of the CXCR3/CXCL10 axis ameliorates inflammation caused by immunoproteasome dysfunction, JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Ming-Shu Mo, .et al. Dopaminergic neurons show increased low-molecular-mass protein 7 activity induced by 6-hydroxydopamine in vitro and in vivo, Transl Neurodegener, 2018, 7: 19 PMID: 30128145
- Ohkusu-Tsukada K, .et al. The Role of Proteasome Inhibitor MG132 in 2,4-Dinitrofluorobenzene-Induced Atopic Dermatitis in NC/Nga Mice, Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Arimochi H, .et al. Differentiation of preadipocytes and mature adipocytes requires PSMB8, Sci Rep, 2016, May 26;6:26791 PMID: 27225296
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Verteporfin

Catalog No. A12658
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YAP 抑制剂

Verteporfin是抑制TEAD-YAP缔合和YAP诱导的肝过度生长的小分子。它也是一种有效的第二代光敏剂，衍生自卟啉。了解更多

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- Po-Ju Lee, .et al. Epstein-Barr viral product-containing exosomes promote fibrosis and nasopharyngeal carcinoma progression through activation of YAP1/FAPα signaling in fibroblasts, J Exp Clin Cancer Res, 2022, Aug 20;41(1):254 PMID: 35986369
- Wang Y, .et al. Verteporfin inhibits lipopolysaccharide-induced inflammation by multiple functions in RAW 264.7 cells, Toxicol Appl Pharmacol, 2019, 2019 Dec 5;387:114852 PMID: 31812773
- Abe T, .et al. Role of YAP Activation in Nuclear Receptor CAR-Mediated Proliferation of Mouse Hepatocytes, Toxicol Sci, 2018, Oct 1;165(2):408-419 PMID: 29893953
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CHIR-090

Catalog No. A12365
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LpxC 抑制剂?

CHIR-090是一种有效，缓慢，亲和力强的 LpxC 脱乙酰酶抑制剂。它与 E. coli LpxC 结合的 Ki 值为 4.0 nM。了解更多

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Cilengitide

Catalog No. A12372
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Integrin 抑制剂

Cilengitide是一种具有潜在抗肿瘤活性的环状精氨酸-甘氨酸-天冬氨酸肽。西仑吉肽结合并抑制α(v)β(3)和α(v)β(5)整联蛋白的活性，从而抑制内皮细胞-细胞相互作用、内皮细胞-基质相互作用和血管生成。了解更多

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- Marion Bouvet, .et al. Anti-integrin αv therapy improves cardiac fibrosis after myocardial infarction by blunting cardiac PW1+ stromal cells, Sci Rep, 2020, 10: 11404 PMID: 32647159
- Rosalie Richards, .et al. 4D imaging and analysis of multicellular tumour spheroid cell migration and invasion, bioRxiv, 2018, 15 Oct 2018
- Hiroki Kanazawa, .et al. Canstatin inhibits hypoxia-induced apoptosis through activation of integrin/focal adhesion kinase/Akt signaling pathway in H9c2 cardiomyoblasts, PLoS One, 2017, 12(2): e0173051 PMID: 28235037
- Yasuda J, .et al. T3 peptide, a fragment of tumstatin, stimulates proliferation and migration of cardiac fibroblasts through activation of Akt signaling pathway, Naunyn Schmiedebergs Arch Pharmacol, 2017, Nov;390(11):1135-1144 PMID: 28785775
- Yasuda J, .et al. T3 peptide, an active fragment of tumstatin, inhibits H2O2-induced apoptosis in H9c2 cardiomyoblasts, Eur J Pharmacol, 2017, Jul 15;807:64-70 PMID: 28457922
- Hsian-Yu Wang, .et al. Non-small-cell lung cancer cells combat epidermal growth factor receptor tyrosine kinase inhibition through immediate adhesion-related responses, Onco Targets Ther, 2016, 9: 2961-2973 PMID: 27284246
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Z-VAD-FMK

Catalog No. A12373
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Pan Caspase 抑制剂

Z-VAD-FMK是一种细胞可渗透、不可逆的泛胱天蛋白酶抑制剂。体外抑制肿瘤细胞caspase加工和凋亡诱导(IC50 = 0.0015 - 5.8 mM)。活跃在体内。了解更多

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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
- Kaori Kanemaru, .et al. Plasma membrane phosphatidylinositol (4,5)-bisphosphate is critical for determination of epithelial characteristics, Nat Commun, 2022, May 9;13(1):2347 PMID: 35534464
- Chie Ishikawa, .et al. Exportin-1 is critical for cell proliferation and survival in adult T cell leukemia, Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
- Aida Falgas, .et al. A diphtheria toxin-based nanoparticle achieves specific cytotoxic effect on CXCR4 + lymphoma cells without toxicity in immunocompromised and immunocompetent mice, Biomed Pharmacother, 2022, Jun;150:112940 PMID: 35421785
- Sumire Suzuki, .et al. Lysosome-targeted drug combination induces multiple organelle dysfunctions and non?canonical death in pancreatic cancer cells, Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Lina Y Abou Zeid, .et al. Caspase-mediated cleavage of miRNA processing proteins Drosha, DGCR8, Dicer, and TRBP2 in heat-shocked cells and its inhibition by HSP70 overexpression, Cell Stress Chaperones, 2022, Jan;27(1):11-25 PMID: 34719748
- Kosar Jabbari, .et al. Protein Ligands in the Secretome of CD36+ Fibroblasts Induce Growth Suppression in a Subset of Breast Cancer Cell Lines, Cancers (Basel), 2021, Sep 8;13(18):4521 PMID: 34572749
- Xiaoyue Deng, .et al. Setd1a Plays Pivotal Roles for the Survival and Proliferation of Retinal Progenitors via Histone Modifications of Uhrf1, Invest Ophthalmol Vis Sci, 2021, May 3;62(6):1 PMID: 33938913
- Liqun Zhao, .et al. Rictor, an essential component of mTOR complex 2, undergoes caspase-mediated cleavage during apoptosis induced by multiple stimuli, Apoptosis, 2021, Apr 27 PMID: 33905036
- Sofia Giacosa, .et al. Cooperative Blockade of CK2 and ATM Kinases Drives Apoptosis in VHL-Deficient Renal Carcinoma Cells through ROS Overproduction, Cancers (Basel), 2021, Feb 2;13(3):576 PMID: 33540838
- Hannes Schmid, .et al. Human invariant natural killer T cells promote tolerance by preferential apoptosis induction of conventional dendritic cells, Haematologica, 2021, Jan 14 PMID: 33440919
- 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
- El-Ashmawy NE, .et al. Modulatory Effect of Silymarin on Apoptosis in Testosterone -Induced Benign Prostatic Hyperplasia in Rats, Pathol Oncol Res, 2020, Jan 4 PMID: 31902118
- Schneider D, .et al. The E3 ubiquitin ligase RNF40 suppresses apoptosis in colorectal cancer cells, Clin Epigenetics, 2019, Jul 2;11(1):98 PMID: 31266541
- Fujiki K, .et al. Blockade of ALK4/5 signaling suppresses cadmium- and erastin-induced cell death in renal proximal tubular epithelial cells via distinct signaling mechanisms, Cell Death Differ, 2019, Feb 25 PMID: 30804470
- T Yamamoto, .et al. Mycoplasma pneumoniae protects infected epithelial cells from hydrogen peroxide-induced cell detachment, Cell Microbiol, 2019, 2019 PMID: 30702185
- Maeda N, .et al. Glucocorticoids potentiate the inhibitory capacity of programmed cell death 1 by up-regulating its expression on T cells, J Biol Chem, 2019, Nov 13. pii: jbc.RA119.010379 PMID: 31723031
- Miyazawa S, .et al. Vitamin K2 induces non-apoptotic cell death along with autophagosome formation in breast cancer cell lines, Breast Cancer, 2019, Oct 17 PMID: 31625014
- Yeh HT, .et al. Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells, Eur J Pharmacol, 2019, Sep 10;863:172658 PMID: 31518562
- D. Bosc, .et al. A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B, Sci Rep, 2018, 8: 11653 PMID: 30076329
- Tsukamoto H, .et al. Lipopolysaccharide (LPS)-binding protein stimulates CD14-dependent Toll-like receptor 4 internalization and LPS-induced TBK1-IKKε-IRF3 axis activation, J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Hiroshi Kuribayashi, .et al. Roles of Nmnat1 in the survival of retinal progenitors through the regulation of pro-apoptotic gene expression via histone acetylation, Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529
- Matsuo J, .et al. Activation of caspase-3 during Chlamydia trachomatis-induced apoptosis at a late stage, Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068
- Orly Ravid, .et al. Blood-Brain Barrier Cellular Responses Toward Organophosphates: Natural Compensatory Processes and Exogenous Interventions to Rescue Barrier Properties, Front Cell Neurosci, 2018, 12: 359 PMID: 30459557
- Im E, .et al. Luteolin induces caspase-dependent apoptosis via inhibiting the AKT/osteopontin pathway in human hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166
- Szalai P, .et al. Nonlinear relationship between ER Ca2+ depletion versus induction of the unfolded protein response, autophagy inhibition, and cell death, Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424
- Im E, .et al. Dihydroartemisinin induced caspase-dependent apoptosis through inhibiting the specificity protein 1 pathway in hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513
- Iriyama N, .et al. The cyclin-dependent kinase 4/6 inhibitor, abemaciclib, exerts dose-dependent cytostatic and cytocidal effects and induces autophagy in multiple myeloma cells, Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
- Birte Plitzko, .et al. The natural product mensacarcin induces mitochondrial toxicity and apoptosis in melanoma cells, J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
- Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
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Salubrinal

Catalog No. A12676
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eIF2α dephosphorylation 抑制剂

Salubrinal是细胞磷酸酶复合物的可渗透细胞的选择性抑制剂，可将真核翻译起始因子2亚基α（eIF2α）磷酸化。保护细胞免受内质网应激诱导的细胞凋亡（EC50?15 μM）。了解更多

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- Gregory R. Kardos, .et al. Salubrinal in Combination With 4E1RCat Synergistically Impairs Melanoma Development by Disrupting the Protein Synthetic Machinery, Front Oncol, 2020, 10: 834 PMID: 32637352
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LX-4211

Catalog No. A12680
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SGLT 抑制剂?

LX4211是双重SGLT1/SGLT2抑制剂。了解更多

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JNJ-28312141

Catalog No. A12687
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CSF1R 抑制剂

JNJ-28312141是一种口服活性CSF1R抑制剂（Colony-stimulating factor-1受体，CRF1R），也是一种FLT3抑制剂。CSF1R在许多肿瘤中表达，是巨噬细胞的生长因子并介导破骨细胞分化。JNJ-28312141代表一种在急性髓样白血病中以及在依赖CSF-1的巨噬细胞和破骨细胞有助于肿瘤生长和骨骼事件的环境中具有潜在治疗活性的新药物。了解更多

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Pacritinib (SB1518)

Catalog No. A12694
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JAK2/FLT3 抑制剂

Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。了解更多

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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
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SCH900776 (S-isomer)

Catalog No. A12703
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CHK1 抑制剂

SCH900776 (S-isomer)是靶向细胞周期检查点激酶1（Chk1）抑制剂，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。具有潜在的放射增敏和化学增敏活性。了解更多

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GSK 2334470

Catalog No. A12767
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PDK1 抑制剂

GSK 2334470是一种有效的3-磷酸肌醇依赖性蛋白激酶（PDK1）抑制剂（IC50?10 nM）。了解更多

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EPZ-5676 (Pinometostat)

Catalog No. A12735
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DOT1L 抑制剂?

EPZ-5676 (Pinometostat)是组蛋白甲基转移酶的小分子抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Yoo H, .et al. Epigenetic priming by Dot1l in lymphatic endothelial progenitors ensures normal lymphatic development and function, Cell Death Dis, 2020, Jan; 11(1): 14 PMID: 31908356
- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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LGK-974

Catalog No. A12816
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PORCN 抑制剂

LGK974是高效，选择性和口服生物利用性的豪猪抑制剂（Wnt信号拮抗剂），在Wnt信号报告基因测定和豪猪结合测定中IC50 <1 nM。了解更多

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- A-Ri Cho, .et al. RNF43 R117fs mutant positively regulates Wnt/β-catenin signaling by failing to internalize FZD expressed on the cell surface, Sci Rep, 2022, Apr 29;12(1):7013 PMID: 35487932
- Yang JM, .et al. LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway, Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
- E Lemieux, .et al. Oncogenic KRAS signalling promotes the Wnt/β-catenin pathway through LRP6 in colorectal cancer, Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
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DMH-1

Catalog No. A12820
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ALK2 抑制剂

DMH-1是骨形态发生蛋白（BMP）ALK2受体的选择性抑制剂（IC50 = 108 nM）。了解更多

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- Teresa Rayon, .et al. Species-specific pace of development is associated with differences in protein stability, Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498
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SCH772984

Catalog No. A12824
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ERK 抑制剂

SCH772984是一种新型的ERK1/2特异性抑制剂，IC50分别为4 nM和1 nM。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Yajun Li, .et al. Urolithin B suppressed osteoclast activation and reduced bone loss of osteoporosis via inhibiting ERK/NF-??B pathway, Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Sergey A. Dyshlovoy, .et al. Activity of New Synthetic (2-Chloroethylthio)-1,4-naphthoquinones in Prostate Cancer Cells, Pharmaceuticals, 2021, 14(10), 949
- Sergey A Dyshlovoy, .et al. Marine alkaloid monanchoxymycalin C: a new specific activator of JNK1/2 kinase with anticancer properties, Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- Guo X, .et al. PDGF-induced migration of synthetic vascular smooth muscle cells through c-Src-activated L-type Ca2+ channels with full-length CaV1.2 C-terminus, Pflugers Arch, 2018, Jun;470(6):909-921 PMID: 29441404
- Takuya Hasegawa, .et al. ErbB2 signaling epigenetically suppresses microRNA-205 transcription via Ras/Raf/MEK/ERK pathway in breast cancer, FEBS Open Bio, 2017, Aug; 7(8): 1154-1165 PMID: 28781955
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GDC-0032 (Taselisib)

Catalog No. A12831
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PI3K 抑制剂

GDC-0032 (Taselisib)是有效的下一代PI3抑制剂，靶向PI3α。了解更多

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TCS ERK 11e (VX-11e)

Catalog No. A12505
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ERK2 抑制剂

TCS ERK 11e (VX-11e)是一种有效且选择性的细胞外信号相关激酶2（ERK2）抑制剂（ERK2，GSK-3，Aurora激酶A和Cdk2的Ki值分别<2、395、540和852 nM）。有效阻断HT29细胞的增殖（IC50 = 48 nM）。了解更多

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- Qi-sang Guo, etc. Involvement of FAK-ERK2 signaling pathway in CKAP2-induced proliferation and motility in cervical carcinoma cell lines. Sci Rep. 2017; 7: 2117.
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PP1

Catalog No. A12724
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Src 抑制剂

PP1是Src家族酪氨酸激酶的有效抑制剂。抑制p56lck和p59fynT（IC50值分别为5和6 nM）。在ZAP-70和JAK2上显示的选择性> 8000倍。还适度抑制p38，CSK，PDGF受体，RET衍生的癌蛋白，c-Kit和Bcr-Abl。了解更多

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PP2

Catalog No. A12723
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Src 抑制剂

PP2是Src家族酪氨酸激酶的选择性抑制剂。抑制p56lck和p59fynT（IC50值分别为4和5 nM）。在ZAP-70和JAK2上显示的选择性> 10000倍。中度抑制CSK（IC50 = 0.73μM）。了解更多

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IWR-1-endo

Catalog No. A12737
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Wnt 抑制剂

IWR-1-endo是Wnt应答的有效抑制剂，可阻断基于细胞的Wnt /β-catenin途径报道分子应答，IC50值为180 nM。 Wnt蛋白与细胞表面的受体结合，启动信号级联反应，从而导致β-catenin激活基因转录。了解更多

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- Charles A.Herring, .et al. Human prefrontal cortex gene regulatory dynamics from gestation to adulthood at single-cell resolution, Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
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LY2090314

Catalog No. A12741
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GSK-3 抑制剂

LY2090314是糖原合酶激酶3（GSK-3）的有效抑制剂，在许多途径中起重要作用，包括蛋白质合成的起始，细胞增殖，细胞分化和凋亡。了解更多

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- Yuki Shimizu, .et al. GSK3 inhibition circumvents and overcomes acquired lorlatinib resistance in ALK-rearranged non-small-cell lung cancer, NPJ Precis Oncol, 2022, Mar 17;6(1):16 PMID: 35301419
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SC-514

Catalog No. A12746
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IκB/IKK 抑制剂

SC-514是一种具有口服活性的，具有ATP竞争性的IKKβ抑制剂（IC50 = 3-12μM），其选择性是JNK，p38，MK2和ERK等28种其他激酶的10倍以上。了解更多

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QNZ (EVP4593)

Catalog No. A12748
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NF-κB 抑制剂

QNZ抑制转录因子NF-κB的激活，已被用于研究NF-κB信号传导。了解更多

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UPF 1069

Catalog No. A12750
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PARP2 抑制剂

UPF 1069是一种选择性聚（ADP-核糖）聚合酶（PARP）2抑制剂（PARP-2和PARP-1的IC50值分别为0.3和8.0μM）。了解更多

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LDE225 Diphosphate

Catalog No. A12774
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Smoothened 抑制剂

LDE225 Diphosphate 是一种具有潜在抗肿瘤活性的口服生物利用小分子平滑（Smo）拮抗剂。抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。了解更多

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Crisaborole (AN2728)

Catalog No. A12776
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PDE4 抑制剂?

AN2728是一种局部给药的含硼抗炎化合物，可抑制PDE4活性，从而抑制TNFalpha，IL-12，IL-23和其他细胞因子的释放。抑制PDE4的 IC50 值为0.49 μM。了解更多

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Freselestat (ONO-6818)

Catalog No. A12780
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neutrophil elastase 抑制剂

Freselestat是一种有效的嗜中性粒细胞弹性蛋白酶抑制剂。在模拟体外循环过程中，Freselestat减少了炎症介质。 ONO-6818显着降低了白介素8和C5b-9的产量。在再循环期间，ONO-6818不能调节CD11b和L-选择素的变化。了解更多

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GSK2606414

Catalog No. A12792
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PERK 抑制剂

GSK2606414是口服有效的选择性PERK抑制剂，IC50为0.4 nM。了解更多

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- Linhao Xu, .et al. Suppression of CHOP Reduces Neuronal Apoptosis and Rescues Cognitive Impairment Induced by Intermittent Hypoxia by Inhibiting Bax and Bak Activation, Neural Plasticity, 2021, 23 Aug
- Takashi Shimizu, .et al. PERK inhibition attenuates vascular remodeling in pulmonary arterial hypertension caused by BMPR2 mutation, Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333
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GSK2578215A

Catalog No. A12798
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LRRK2 kinase 抑制剂

GSK2578215A是一种有效的富含亮氨酸的重复激酶2（LRRK2）抑制剂（LRRK2 [G2019S]突变体和野生型LRRK2的IC50值分别为8.9和10.1 nM）。了解更多

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CEP33779

Catalog No. A12808
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JAK2 抑制剂

CEP33779是选择性JAK2抑制剂，IC50为1.8 nM。了解更多

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AZD1080

Catalog No. A12819
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GSK3 抑制剂

AZD1080是一种新型GSK3抑制剂，可消除啮齿动物大脑中的突触可塑性缺陷，并在人类中表现出外周靶标参与。了解更多

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- Shengzhong Liu, .et al. STAT1-avtiviated LINC00961 regulates myocardial infarction by the PI3K/AKT/GSK3?? signaling pathway, J Cell Biochem, 2019, 2019
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LDN-212854

Catalog No. A12821
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BMP receptor 抑制剂

LDN-212854是一种ALK2偏爱的BMP I型受体激酶抑制剂。了解更多

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HSP-990

Catalog No. A12850
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HSP90 抑制剂

HSP990是人热休克蛋白90（Hsp90）的口服生物利用抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。具有潜在的抗肿瘤活性。了解更多

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- Michael Heider, .et al. The IMiD target CRBN determines HSP90 activity toward transmembrane proteins essential in multiple myeloma, Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422

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