AS2521780

Research use only, not for human use.

AS2521780 is a?potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 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

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1214726-89-2

547.766

C30H41N7OS

>98% (HPLC)

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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