RO-5963

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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。

RO-5963 

RO-5963 是 p53-MDM2 和 p53-MDMX 互相作用的双抑制剂，IC50 值分别约为 17 nM 和 24 nM。

RO-5963

RO-5963 Chemical Structure

CAS No. : 1416663-77-8

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生物活性

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1].

IC50 & Target

IC50: ~17 nM (p53-MDM2), ~24 nM (p53-MDMX)[1]
体外研究
(In Vitro)

RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines[1].
RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels[1].

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

Apoptosis Analysis[1]

Cell Line: ZR75-30, MCF7 cells
Concentration: 10, 20 μM
Incubation Time: 48 hours
Result: Potently showed apoptotic activity.

Western Blot Analysis[1]

Cell Line: LNCap, U2OS, RKO, A489, 22Rv1, HCT116, H460, LOX, MCF7, A549, G401 cells
Concentration: 10 μM
Incubation Time: 24 hour
Result: Effectively activated p53 and elevated p21 and MDM2 levels.

分子量

518.90

Formula

C24H21ClF2N4O5
CAS 号

1416663-77-8
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]. Graves B, et al. Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93.

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