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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 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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货号: HY-12000
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