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AS2521780

Catalog No.GC31959

AS2521780 est un nouvel inhibiteur sélectif de PKCθ avec une IC50 de 0,48 nM.

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AS2521780 Chemical Structure

Cas No.: 1214726-89-2

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 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].

[1]. Fukahori H, et al. Effect of AS2521780, a novel PKCθ selective inhibitor, on T cell-mediated immunity. Eur J Pharmacol. 2014 Dec 15;745:217-22.

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