Description
AS2521780 is apotent, selective, orally bioavailable PKCtheta inhibitor that inhibits combinant human PKCtheta enzyme with IC50 of 0.48nM, >30-fold higher than other PKC isoforms; also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84nM); suppresses CD3/CD28-induced IL-2 gene transcription (IC50=14nM) in Jurkat T cells and proliferation of human primary T cells (IC50=17nM), also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency; potentially ameliorate T cell-mediated autoimmune diseases in vivo models