NSC66811

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Chemical Structure| 6964-62-1 同义名 : -
CAS号 : 6964-62-1
货号 : A183021
分子式 : C23H20N2O
纯度 : 98%
分子量 : 340.418
MDL号 : -
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(308.44 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
动物实验配方：
生物活性
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 Ki 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.38mL

5.88mL

2.94mL
参考文献

[1]Modulation of the pentose phosphate pathway alters phase I metabolism of testosterone and dextromethorphan in HepG2 cells

[2]Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.

[3]Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development