AG490 | MedChemExpress (MCE)

AG490 | MedChemExpress (MCE)

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AG490

CAS No. : 133550-30-8

MCE 国际站:AG490

产品活性:AG490 (Tyrphostin AG490) 是酪氨酸激酶抑制剂,其抑制EGFRStat-3JAK2/3

研究领域:JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  Stem Cell/Wnt  |  Epigenetics  |  Autophagy

作用靶点:EGFR  |  STAT  |  JAK  |  Autophagy

In Vitro: AG490 inhibits the activation of Stat-3 by selectively blocking JAK2. AG490 is used to selectively inhibit JAK/Stat-3 activation. At a dose of 10 μM, Stat-3 phosphorylation is decreased by >95% and cell viability is maintained. AG490 at a dose of 10 μM results in >95% decrease in pStat-3 in EGF-stimulated A431 cells with no effect on Stat-3 mass. AG-490 is a potent inhibitor of the JAK3/STAT, JAK3/AP-1, and JAK3/MAPK pathways and their cellular consequences. AG-490 abolishes IL-2-inducible [3H]thymidine incorporation in a dose-dependent manner, displaying an IC50 of 25 μM. AG-490 potently inhibits IL-2-mediated proliferation in T cells, results distinct from previous studies that showed this agent induced apoptosis in ALL cells while exerting apparently no effects on the growth of mitogen-stimulated normal T cells.

In Vivo: AG490 significantly inhibits the development of type 1 diabetes (T1D) (p = 0.02, p = 0.005; at two different time points). Monotherapy of newly diagnosed diabetic NOD mice with AG490 (1 mg/mouse) markedly results in disease remission in treated animals (n=23) in comparision to the absolute inability (0%; 0/10, p=0.003, Log-rank test) of DMSO and sustained eugluycemia is maintained for several months following drug withdrawal. AG490 (1-10 µg) significantly attenuates ʎ-carrageenan-induced thermal hyperalgesia in a dose-dependent manner. AG490 also reduces mechanical hyperalgesia.

相关产品:Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-diabetic Compound Library  |  Anti-Hepatitis C Virus Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Transcription Factor-Targeted Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Anti-Prostate Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Cysteine Targeted Covalent Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  JAK-IN-20  |  Stafia-1-dipivaloyloxymethyl ester  |  JAK1-IN-9  |  EGFR/HER2/CDK9-IN-2  |  Lapatinib ditosylate  |  BMS-690514  |  AT9283  |  RO495  |  TK4b  |  Erlotinib-d6 hydrochloride  |  JAK-IN-17  |  EGFR/CDK2-IN-1  |  (E/Z)-Zotiraciclib  |  JBJ-04-125-02  |  EGFR-IN-22  |  JAK-IN-10  |  EGFR-IN-34  |  Epertinib  |  Ponezumab  |  Niclosamide monohydrate  |  (3R,4S)-Tofacitinib  |  JAK3/BTK-IN-6  |  Erlotinib Hydrochloride  |  EGFR-IN-36  |  EGFR-IN-62  |  Genistein  |  Tyk2-IN-5  |  Panitumumab (anti-EGFR)  |  Brevilin A

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