AS2521780 |CAS:1214726-89-2 Probechem Biochemicals

Chemical Structure : AS2521780

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AS2521780 (AS 2521780;AS-2521780)

货号: PC-60994Not For Human Use, Lab Use Only.

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.

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生物&药学活性

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.
AS2521780 also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84 nM).
AS2521780 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).
AS2521780 also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency.
AS2521780 potentially ameliorate T cell-mediated autoimmune diseases in vivo models.

物理化学性质&存储条件

分子量	547.766
分子式	C30H41N7OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Fukahori H, et al. Eur J Pharmacol. 2014 Dec 15;745:217-22.

AS2521780 (AS 2521780;AS-2521780)

生物&药学活性

物理化学性质&存储条件

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AS2521780 (AS 2521780;AS-2521780)

生物&药学活性

物理化学性质&存储条件

参考文献

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