化学性质:
规格 | 10mg 50mg |
CAS | 431979-47-4 |
别名 |
|
化学名 | methyl 2-[2-chloro-6-ethoxy-4-[(3-methyl-5-oxo-1-phenylpyrazol-4-ylidene)methyl]phenoxy]acetate |
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°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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].
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