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PS315
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PS315图片
CAS NO:1221964-50-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

PS315, a derivative of PS48 (HY-15967), is an allostericPKCinhibitor 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 ofPKCζ(IC50=10 μM) andPKCη(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].

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.