SJ-172550 是 MDMX 的小分子抑制剂,EC50为5 μM。
产品描述
SJ-172550 is a small molecule inhibitor of MDMX (EC50: 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].
Cas No.
431979-47-4
分子式
C22H21ClN2O5
分子量
428.87
储存和溶解度
DMSO:33.33 mg/mL (77.72 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years