CAS:6964-62-1NSC 66811

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NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM which can disrupt MDM2-p53 interaction and activate p53 function.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

6964-62-1

储存条件

分子式

C23H20N2O

运输

蓝冰

分子量

340.42

别名

溶解度

DMSO	75.0 mg/mL (220.3 mM)
Water	insoluble

动物实验配方

生物活性

靶点 MDM2

Ki:120nM
描述Tumor suppressor p53 is a powerful growth suppressive and pro-apoptotic protein that plays a central role in protectionfrom tumor development. The overproduction of MDM2 (murine double minute 2), the primary negative regulator of p53, effectively disables p53 function^[3]. NSC 66811, a novel inhibitor of the MDM2-p53 interaction, binds to MDM2 with a K_i of 120 nM and activates p53 in cancer cells with a mechanism of action consistent with targeting the MDM2-p53 interaction^[2]. HepG2 cells were treated for 24 h with NSC 66811 (5 and 25 μmol/L), and the p53 mRNA levels were upregulated by NSC 66811 without affecting the CYP expression. Addition of the p53 activator NSC 66811 (3, 10, 25 μmol/L) in HepG2 cells dose-dependently inhibited the metabolism of DEM (dextromethorphan) and TEST (testosterone). For CYP3A4, the metabolism of TEST was reduced by 1.5-, 2.9-, and 6.8-fold with 3, 10, and 25 μmol/L of NSC 66811, respectively, indicating that p53 activation decreased the metabolic efficiency through both CYP2D6 and 3A4^[1].
作用机制NSC 66811 mimics three p53 residues critical in the binding to MDM2^[2].