AS2521780

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AS2521780

CAS No. : 1214726-89-2

MCE 国际站：AS2521780

产品活性：AS2521780是新颖的 PKCθ 选择性抑制剂，IC₅₀ 值为0.48 nM。

研究领域：Epigenetics  |  TGF-beta/Smad

作用靶点：PKC

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.

In Vivo: AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis.

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