Name | Nutlin-3b |
Description | Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a. |
Cell Research | MTT assay(Only for Reference) |
Kinase Assay | 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 |
In vitro | 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] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 93 mg/mL (159.9 mM) Ethanol : 93 mg/mL (159.9 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
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Keywords | 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 |
Inhibitors Related | Milademetan | NSC697923 | XI-006 | PYZD-4409 | Nutlin-3 | NAcM-OPT | PYR-41 | NSC232003 | NAE-IN-M22 | Indole-3-carbinol | Idasanutlin | RITA |
Related Compound Libraries | Apoptosis Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Pyroptosis Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |