化合物Nutlin-3a T6023
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Product IntroductionBioactivity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，
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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
相关产品: Ceramide (Egg, Chicken) | Psoralen | Perifosine | Neferine | Cl-amidine hydrochloride | (-)-Zeylenol | Vitamin K4 | Hesperidin | Anticancer agent 133 | Tubastatin A Hydrochloride
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
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
相关产品: Ceramide (Egg, Chicken) | Psoralen | Perifosine | Neferine | Cl-amidine hydrochloride | (-)-Zeylenol | Vitamin K4 | Hesperidin | Anticancer agent 133 | Tubastatin A Hydrochloride
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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