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AG490

CAS No. : 133550-30-8

MCE 站：AG490

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

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 ?g) significantly attenuates ?-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  |  Diabetes Related 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  |  Gefitinib  |  Trastuzumab  |  Stattic  |  Erlotinib  |  Cetuximab  |  Upadacitinib  |  Fludarabine  |  Genistein  |  AS1517499  |  Niclosamide  |  Artesunate  |  Homoharringtonine  |  AG-1478  |  TPCA-1  |  Colivelin TFA  |  Cryptotanshinone  |  Napabucasin  |  Pimozide  |  STAT5-IN-1  |  Pertuzumab  |  C188-9  |  BI-4020  |  AT9283  |  Gandotinib  |  Scutellarin  |  NSC 228155  |  Lestaurtinib  |  Pelitinib

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