431979-47-4|SJ-172550|CsnPharm

CAS No.: 431979-47-4

SJ-172550 Catalog No. CSN18271

Synonyms: MDMX Inhibitor II

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

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400-920-2911

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技术信息

生物活性

描述The p53 pathway is disrupted every human tumor. The wt p53-induced actin protein levels are modulated by natural (MDM2 and MDMX) and chemical (pifithrin-α, nutlin-3a and SJ-172550) regulators of p53 activity. SJ-172550 was previously discovered in a biochemical high throughput screen for inhibitors of the interaction of MDMX and p53 and characterized as a reversible inhibitor with an EC50 value of 4.3 µM. It acts through a complicated mechanism in which the compound forms a covalent but reversible complex with MDMX and locks MDMX into a conformation^[3]. SJ 172550 induces apoptosis, increases p53 target gene expression, and causes p53-dependent cell death in retinoblastoma cells^[4].
参考文献

[1] Bista M, Smithson D, et al. On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53. PLoS One. 2012;7(6):e37518.
[2] Reed D, Shen Y, et al. Identification and characterization of the first small molecule inhibitor of MDMX. J Biol Chem. 2010 Apr 2;285(14):10786-96.
[3] 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).
[4] Reed, D. et al. Identification and Characerization of the First Small Molecule Inhibitor of MDMX. JBC. 2010. 285(14).

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3317 mL
- 11.6587 mL
- 23.3173 mL
- 5 mM
- 0.4663 mL
- 2.3317 mL
- 4.6635 mL
- 10 mM
- 0.2332 mL
- 1.1659 mL
- 2.3317 mL

技术信息

CAS号

431979-47-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H21ClN2O5

运输

蓝冰

分子量

428.87

别名

MDMX Inhibitor II

溶解度

DMSO	30.0 mg/mL (70.0 mM) warming

动物实验配方

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