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Decernotinib
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Decernotinib
CAS No. : 944842-54-0
MCE 站:Decernotinib
产品活性:Decernotinib 是一种有效的,可口服的 JAK3 抑制剂,对 JAK3,JAK1,JAK2 和 TYK2 的 Ki 值分别为 2.5,11,13 和 11 nM。
研究领域:Epigenetics | Stem Cell/Wnt | JAK/STAT Signaling
作用靶点:JAK
In Vitro: Decernotinib (VX-509) is a potent JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively. Decernotinib potently blocks T-cell proliferation with a mean IC50 of 170 ± 101 nM, and inhibits IL-2-stimulated T-cell proliferation (IC50, 140 and 400 nM). VX-509 is also cytotoxic to B-cell in response to CD40L and IL-4 (IC50, 50 nM).
In Vivo: Decernotinib (VX-509, 10, 25, or 50 mg/kg, p.o.) significantly and dose-dependently inhibits the increases in ankle diameter and paw weight occuring in response to collagen injections in rats. Decernotinib potently alleviates cartilage damage and bone resorption in rats. Decernotinib (10, 25, or 50 mg/kg, p.o., b.i.d.) suppresses ear edema in a mouse model of delayed-type hypersensitivity.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Ruxolitinib | AG490 | Tofacitinib | Baricitinib | Deucravacitinib | Upadacitinib | Fedratinib | Peficitinib | Pacritinib | Filgotinib | Zotiraciclib | WP1066 | Itacitinib | Momelotinib | Delgocitinib | Ritlecitinib | Abrocitinib | AZD-1480 | AT9283 | Brepocitinib P-Tosylate | CHZ868 | Gandotinib | Cerdulatinib | JANEX-1 | Lestaurtinib | Cucurbitacin I | Ropsacitinib
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