VX-509 |
カタログ番号GC40761 |
VX-509は、JAK3の選択的阻害剤であり、酵素アッセイにおけるKi値は2.5 nMであり、JAK3活性に依存する細胞アッセイにおけるIC50値は50〜170 nMであり、他のJAKアイソタイプに対して測定可能な活性を示しません。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 944842-54-0
Sample solution is provided at 25 µL, 10mM.
Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.
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)[1].
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[1].
References:
[1]. Mahajan S, et al. VX-509 is a potent and selective Janus kinase 3 (JAK3) inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther. 2015 Mar 11. pii: jpet.114.221176.
Average Rating: 5
(Based on Reviews and 10 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *