AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).

PKCα:160 nM, PKCδ:160 nM, PKCθ:0.48 nM, PKCε:18 nM

AS2521780 suppresses CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and proliferation of human primary T cells and it also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey peripheral blood mononuclear cells with similar potency[1]. AS2521780 exerts potent inhibition of recombinant human PKCθ enzyme activity (IC50=0.48 nM). Which is more than 30-fold higher than that of other PKC isoforms. Further, AS2521780 exerts little or no inhibition on other protein kinases.

AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis[1].