AS2521780 |
| رقم الكتالوجGC31959 |
AS2521780 هو مثبط انتقائي جديد لـ PKCθ مع IC50 من 0.48 نانومتر
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Cas No.: 1214726-89-2
Sample solution is provided at 25 µL, 10mM.
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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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