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Biological Activity:
A p38 MAP kinase inhibitor. VX-702 dose-dependently inhibited the production of IL-6, IL-1β and TNFα (IC₅₀ = 59, 122 and 99 ng/ml, respectively). Pre-incubation of platelets with VX-702 (1 µM) completely or partially inhibited platelet agonist induced p38 activation (IC₅₀= 4 to 20 nM).
References:
1. Goldstein DM et al.Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.J Med Chem53:2345-53 (2010).
2. Kuliopulos A et al.Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation.Thromb Haemost92:1387-93 (2004).