化合物Nutlin-3a T6023

Product Introduction
Bioactivity


英文名: Nutlin-3a

描述: Nutlin-3a ((−)-Nutlin-3) 是 Nutlin-3 的活性对映体，是一种 MDM2抑制剂，可抑制 MDM2-p53相互作用，稳定 p53 蛋白，从而诱导细胞自噬和凋亡，有潜力研究 TP53野生型卵巢癌。

细胞实验: SRB(Only for Reference)

激酶实验: Biacore studies: Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel

体外活性: 用10 μM nutlin-3a孵育7天导致NIH3T3细胞生长抑制> 90％。Nutlin-3α稳定并激活p53基因,剂量依赖性诱导p21的表达。Nutlin-3a取代MDM2结合口袋中的p53,从而释放p53抑制和蛋白酶体降解,导致诱导其下游靶点,细胞周期停滞和凋亡。Nutlin-3A有效地减少S期细胞至0.2-2％,并增加了G1-和G2/M期细胞。Nutlin-3a诱导约60％的SJSA-1和MHM细胞在40小时后发生凋亡,其在60小时后分别进一步增加（分别为85％和65％）。

体内活性: Nutlin-3是体内p53途径的选择性激活剂,对SJSA-1骨肉瘤肿瘤具有高度的有效性.Nutlin-3α以剂量依赖性方式抑制异种移植物生长,其中最高剂量（200 mg/kg）表现出显著的肿瘤缩小.Nutlin-3α治疗对有野生型p53和MDM2基因扩增的肿瘤效果最佳.

存储条件: store at low temperature,keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 58.2 mg/mL (100 mM)
DMSO : 55 mg/mL (94.58 mM)
5% DMSO+95% Saline : 2.91 mg/mL (5 mM, suspension)


关键字: E1 activating enzyme | inhibit | E3 ligating enzyme | p53 | carcinomas | E1/E2/E3 Enzyme | ovarian | Nutlin-3 | Ubiquitin ligase | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | Nutlin 3a | Autophagy | Inhibitor | Nutlin-3a | Nutlin3a | MDM-2/p53 | Rebemadlin | E2 conjugating enzyme | Apoptosis

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相关库: Anti-Aging Compound Library | Glycometabolism Compound Library | Transcription Factor-Targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途