Catalog No.: PC-60994Not For Human Use, Lab Use Only.
AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms.
AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms.
AS2521780 also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84 nM).
AS2521780 suppresses CD3/CD28-induced IL-2 gene transcription (IC50=14 nM) in Jurkat T cells and proliferation of human primary T cells (IC50=17 nM).
AS2521780 also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency.
AS2521780 potentially ameliorate T cell-mediated autoimmune diseases in vivo models.
