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

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

AS2521780 effectively inhibits CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and the proliferation of human primary T cells. Additionally, it impedes concanavalin A-induced cytokine production in rat splenocytes and monkey peripheral blood mononuclear cells with comparable efficacy[1]. The compound demonstrates a potent inhibition of recombinant human PKCθ enzyme activity, with an IC50 value of 0.48 nM, showcasing more than a 30-fold selective inhibition over other PKC isoforms. Moreover, AS2521780 exhibits minimal or no inhibitory effects on other protein kinases.

AS2521780 markedly diminishes paw swelling through a dose-dependent mechanism in a rat model of adjuvant-induced arthritis[1].