Home Apoptosis MDM2/MDMX antagonist Nutlin-3b

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Nutlin-3b MDM2/MDMX antagonist

Cat.No.S8065

Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of this compound as in comparison with opposite (-)-enantiomer Nutlin-3a.
Nutlin-3b MDM2/MDMX antagonist Chemical Structure

Chemical Structure

Molecular Weight: 581.49

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Quality Control

Batch: S806501 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

Chemical Information, Storage & Stability

Molecular Weight 581.49 Formula

C30H30Cl2N4O4

 Storage (From the date of receipt)
CAS No. 675576-97-3 -- Storage of Stock Solutions

Synonyms (+)-Nutlin-3 Smiles CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
MDM2 [1]
13.6 μM
In vitro
Nutlin-3b is useful as a negative control 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. This compound 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 this chemical 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 this compound are indistinguishable from the untreated controls. [1]
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 this compound 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 this chemical is calculated as a percentage of binding in its absence and IC50 is calculated
References

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