PS315

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PS315 

PS315 是 PS48 (HY-15967) 的衍生物，是一种变构性 PKC 抑制剂，可以与 aPKC 的 PIF 口袋结合并诱导活性位点残基 Lys111 置换。PS315 抑制 PKCζ (IC50=10 μM) 和 PKCη (IC50=30 μM) 的全长和催化结构域构建体。PS315 具有抗癌活性。

PS315

PS315 Chemical Structure

CAS No. : 1221964-50-6

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生物活性

PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity[1].

IC50 & Target[1]

PKCζ

10 μM (IC50)

PKCη

30 μM (IC50)

体外研究
(In Vitro)

Preincubation of U937 cells with 5 μM PS315 inhibits TNF-α induced NF-κB activation by 74%, whereas complete inhibition is observed with 10 μM PS315[1].
The small allosteric inhibitor PS315 and the N-terminal region of aPKC both act directly on the PIF-pocket on-off switch. PS315, binding at the PIF-pocket, induces a displacement of the active site residue Lys111, thereby inhibiting the activity of aPKCs by allosterically affecting the catalytic mechanism of the kinase[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

362.85

Formula

C23H19ClO2
CAS 号

1221964-50-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang H, et al. Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound. Chem Biol. 2014 Jun 19;21(6):754-65.

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