"目录号: HY-15335
Nutlin-3b是MDM2/p53抑制剂，IC50为13.6 μM。
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生物活性
Description
Nutlin-3b is a MDM2/p53 antagonist or inhibitor with IC50 of 13.6 μM. Nutlin-3b is a less active enantiomer
IC50& Target
IC50: 13.6 μM (MDM2/p53)
In Vitro
Nutlin-3b is a 150-fold less potent (+)-enantiomer of Nutlin-3 as p53 MDM2 antagonist or inhibitor, in comparison with more potent opposite (-)-enantiomer Nutlin-3a. It is useful as a negative control for non-Mdm2 related cellular activities. 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.
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