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SJ-172550

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Chemical Structure| 431979-47-4 同义名 : MDMX Inhibitor II
CAS号 : 431979-47-4
货号 : A527934
分子式 : C22H21ClN2O5
纯度 : 99%+
分子量 : 428.866
MDL号 : MFCD03142926
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(81.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.32mL

4.66mL

2.33mL
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).