化合物Nutlin-3b T6614

Product Introduction
Bioactivity


英文名: Nutlin-3b

描述: Nutlin-3b ((+)-Nutlin-3) 是一种 p53/MDM2 拮抗剂或抑制剂，IC50为 13.6 μM。它与 MDM2 的结合活性比 Nutlin-3a 低 150 倍。

细胞实验: MTT assay(Only for Reference)

激酶实验: Biacore study: Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the 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. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25°C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculated

体外活性: Nutlin-3b is useful as a negative control s for non-MDM2-related cellular activities. Nutlin-3a induces the expression of MDM2 and p21 (but not p53) only in cells with wild-type p53. Nutlin-3b has no effect regardless of the p53 status of the cells. Only the active enantiomer Nutlin-3a shows a potent antiproliferative activity and clear separation of potency between the cells harboring wild-type p53 and those harboring mutant p53. The potency of Nutlin-3b is much lower in the wild-type p53 cells and nearly identical to the potency of Nutlin-3a against the mutant p53 cells. After 48 hours of exposure to the Nutlin-3a, 45% of the cell population became TUNEL positive, but cells treated with the Nutlin-3b are indistinguishable from the untreated controls. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (159.9 mM)
Ethanol : 93 mg/mL (159.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Nutlin 3b | Inhibitor | MDM-2/p53 | Ubiquitin activating enzyme | Ubiquitin conjugating enzyme | inhibit | E1 activating enzyme | E1/E2/E3 Enzyme | Ubiquitin ligase | E3 ligating enzyme | Nutlin-3 | E2 conjugating enzyme | Nutlin-3b | Nutlin3b

相关产品: RDR03871 | RG7112 | Ganoderic acid X | p53-MDM2-IN-1 | Milademetan | RO8994 | Triptolide | p53-Mdm2 inhibitor 4 | RO-5963 | NSC 66811

相关库: Anti-Aging Compound Library | HIF-1 Signaling Pathway Compound Library | Pyroptosis Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | PPI Inhibitor Library | Autophagy Compound Library | Preclinical Compound Library | Bioactive Compound Library

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