AS2521780

AS2521780 is a novel PKCθ selective inhibitor with an IC₅₀ of 0.48 nM. IC50 & Target:IC50: 0.48 nM (PKCθ)^[1] In Vitro: 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 suppresses CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and proliferation of human primary T cells. AS2521780 also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey peripheral blood mononuclear cells with similar potency^[1]. In Vivo: AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis^[1].