AS2521780

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AS2521780 是一种有效的、选择性的、口服生物可利用的 PKCθ 抑制剂，可抑制人组合 PKCθ 酶，IC50 为 0.48 nM。

AS2521780 is a?potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms; also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84 nM); suppresses CD3/CD28-induced IL-2 gene transcription (IC50=14 nM) in Jurkat T cells and proliferation of human primary T cells (IC50=17 nM), also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency; potentially ameliorate T cell-mediated autoimmune diseases in vivo models.

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.

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

AS 2521780 | AS-2521780

Angiogenesis

PKC

PKC

——

——

1214726-89-2

547.766

C30H41N7OS

>98% (HPLC)

——

N#CC1=CN=C(NCC2=CC=CN=C2SC)N=C1NC[C@]34C[C@]5([H])[C@H](NC[C@H]6CC[C@H](O)CC6)[C@@](C4)([H])CC(C5)C3

4-({[(1R,3R,4s,5S)-4-{[(trans-4-hydroxycyclohexyl) methyl]amino}adamantan-1-yl]methyl}amino)-2-({[2-(methylsulfanyl)pyridin-3-yl]methyl}amino)pyrimidine-5-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years