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NSC 66811
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。
NSC 66811图片
CAS NO:6964-62-1
包装:10mg
市场价:536元

产品介绍
NSC 66811 是一种 MDM2-p53 抑制剂,与 MDM2 结合的 Ki 值为 120 nM。
Cas No.6964-62-1
别名7-(ALPHA-苯胺基苄基)-2-甲基-8-喹啉醇
化学名7-[anilino(phenyl)methyl]-2-methylquinolin-8-ol
Canonical SMILESCC1=NC2=C(C=C1)C=CC(=C2O)C(C3=CC=CC=C3)NC4=CC=CC=C4
分子式C23H20N2O
分子量340.42
溶解度≥ 34 mg/mL in DMSO, ≥ 3.82 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
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

NSC 66811 is a small-molecule inhibitor of the murine double minute 2 (MDM2) p53 interaction with Ki value of 120nM [1].

The N-terminus of p53 and a deep hydrophobic cleft in MDM2 form a short helix between p53 and MDM2. NSC 66811 binds the active site of this cleft. NSC 66811 has a high binding affinity with Ki of 120nM and is 56 times more potent than the natural p53 peptide. The stereoisomers of NSC 66811 mimic the three key residues of p53 (Phe19, Trp26, and Leu26), mediating the interaction with MDM2. NSC 66811 is reported to induce the accumulation of p53, MDM2, and p21cip1/waf proteins in the HCT-116 human colon cancer cell line with wild-type p53. However, NSC 66811 has no effect on the levels for p53, MDM2, and p21cip1/waf protein in the isogenic HCT-116 p53 /cell line [1].

References:
[1] Lu Y, Nikolovska-Coleska Z, Fang X, Gao W, Shangary S, Qiu S, Qin D, Wang S. Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy. J Med Chem. 2006 Jun 29;49(13):3759-62.