VX-702
p38α MAP kinase inhibitor / A potent and selective inhibitor of p38 MAP kinases, p38α MAPK and p38 (KD = 3.7 and 17 nM respectively).1 Inhibits IL-6, IL-1 and TNFα production in LPS-primed blood.1 Inhibits p38 in platelets stimulated by thrombin, collagen or thromboxane agonist U-46619 at 1 uM.2 Provides only modest clinical efficacy in rheumatoid arthritis.3,4 Delays platelet lesions and leads to better maintenance of stored platelets.5
Biochemicals & reagents
745833-23-2
1) Goldstein et al. (2010), Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders; J. Med. Chem., 53 2345 2) Kuliopulos et al. (2004), Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation; Thromb. Haemostasis, 92 1387 3) Damianov et al. (2009), Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies; Arthrit. Rheumat., 60 1232 4) Ding et al. (2006), Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome; Curr. Opin. Investig. Drugs, 7 1020 5) Scripchenko et al. (2013), An inhibition of p38 mitogen activated protein kinase delays the platelet storage lesion; PLoS One, 8(8)e 70732
-20°C
TARGET: Kinase -- PATHWAY: TNF; Cytokine; Coagulation -- DISEASE AREA: Inflammation