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SJ-172550

SJ-172550 是 MDMX 的小分子抑制剂，EC50为5 μM。

CAS号

431979-47-4

分子式

C22H21ClN2O5

主要靶点

E1/E2/E3 Enzyme|Mdm2

仅限科研使用

Cat No : CM05045

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Synonyms

验证数据展示

  • CAS No.: 431979-47-4

    SJ-172550
    CAS#: 431979-47-4

产品信息

SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).

CAS号 431979-47-4
分子式 C22H21ClN2O5
主要靶点 E1/E2/E3 Enzyme|Mdm2
主要通路 泛素化|凋亡
分子量 428.87
纯度 99.87%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

MDMX:5 μM

体外活性

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. 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 effect of SJ-172550 is additive when combined with an MDM2 inhibitor nutlin-3a. The relative stability of this complex is influenced by many factors including the reducing potential of the media, the presence of aggregates [1][2].

溶解度

DMSO:33.33 mg/mL (77.72 mM),Sonification is recommended.

参考文献

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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