货号:A527934
同义名:
MDMX Inhibitor II
SJ-172550是一种小分子 MDMX 抑制剂,可通过竞争性结合阻止野生型 p53 肽与 MDMX 的结合,其 EC50 为 5 μM。


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| 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]. |
| Concentration | Treated Time | Description | References | |
| Weri1 retinoblastoma cells | 20 µM | 20 hours | To test the cytotoxic effect of SJ-172550 on MDMX-amplified retinoblastoma cells, results showed apoptosis and cell cycle exit. | J Biol Chem. 2010 Apr 2;285(14):10786-96 |
| U2OS cells | 10 µM | 72 hours | Evaluate the synergistic effect of SJ-172550 with Nutlin-3a, results showed no synergy | ACS Chem Biol. 2018 Oct 19;13(10):2849-2854 |
| 计算器 | ||||
| 存储液制备 | ![]() |
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 |
|
| CAS号 | 431979-47-4 |
| 分子式 | C22H21ClN2O5 |
| 分子量 | 428.87 |
| SMILES Code | O=C(/C1=C/C2=CC(Cl)=C(OCC(OC)=O)C(OCC)=C2)N(N=C1C)C3=CC=CC=C3 |
| MDL No. | MFCD03142926 |
| 别名 | MDMX Inhibitor II |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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