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SCH 529074
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SCH 529074图片
CAS NO:922150-11-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
SCH 529074 是一种有效且具有口服活性的 p53 激活剂。 SCH 529074 与 p53 DBD(DNA 结合域)特异性和构象依赖性结合,Ki 为 1-2 μM,可饱和。 SCH 529074 恢复突变 p53 功能并中断 HDM2 介导的野生型 p53 泛素化。 SCH 529074 可用于研究非小细胞肺癌 (NSCLC)。
Cas No.922150-11-6
化学名(E)-N1-(2-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4(3H)-ylidene)-N3,N3-dimethylpropane-1,3-diamine
Canonical SMILESCN(CCC/N=C1C2=CC=CC=C2N=C(N\1)CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)C
分子式C31H36Cl2N6
分子量563.56
溶解度25mg/mL in DMSO, 33mg/mL in ethanol, or in DMF
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.[1] SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.

Reference:
[1]. Demma, M., Maxwell, E., Ramos, R., et al. SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. J. Biol. Chem. 285(14), 10198-10212 (2010).