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SJ 172550
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。
SJ 172550图片
CAS NO:431979-47-4
包装与价格：
包装价格(元)
10mg询价
50mg询价

SJ 172550 是一种小分子 MDMX 抑制剂；竞争与 MDMX 结合的野生型 p53 肽，EC50 为 5 μM。
Cas No.431979-47-4
化学名methyl 2-[2-chloro-6-ethoxy-4-[(3-methyl-5-oxo-1-phenylpyrazol-4-ylidene)methyl]phenoxy]acetate
Canonical SMILESCCOC1=C(C(=CC(=C1)C=C2C(=NN(C2=O)C3=CC=CC=C3)C)Cl)OCC(=O)OC
分子式C22H21ClN2O5
分子量428.87
溶解度DMF: 30 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 10 mg/ml,Ethanol: slightly
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.

The p53 pathway is disrupted in virtually every human tumor. SJ-172550 binds the p53-binding pocket of MDMX, thereby displacing p53. SJ-172550 binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified. The effect of SJ-172550 is additive when combined with an MDM2 inhibitor nutlin-3a[1]. SJ-172550 acts through a complicated mechanism in which the compound forms a covalent but reversible complex with MDMX and locks MDMX into a conformation that is unable to bind p53. The relative stability of this complex is influenced by many factors including the reducing potential of the media, the presence of aggregates[2].

References:
[1]. Reed D, et al. Identification and characterization of the first small molecule inhibitor of MDMX. J Biol Chem. 2010 Apr 2;285(14):10786-96.
[2]. Bista M, et al. On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53. PLoS One. 2012;7(6):e37518.

 
 
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