AS2521780 is a novelPKCθselective inhibitor with anIC₅₀of 0.48 nM.

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].

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

547.76

C₃₀H₄₁N₇OS

1214726-89-2

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