MDM2 Antagonist, Nutlin-3, Racemic,1MG,444143-1MGCN,Sigma

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订货号 0BV4532
品牌型号 Sigma 444143-1MGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

General description

A cell-permeable cis-imidazoline compound that acts as a potent and selective MDM2 antagonist (IC50 = 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b) and displays antitumor properties. Activates p53 pathway by binding MDM2 in the p53-binding pocket and inhibits MDM2-p53 interaction. Shown to suppress tumor growth by induction of apoptosis in several cancer cells with wild-type p53 and in xenografted tumor mice. A 10 mM (1 mg/172 µl) solution of MDM2 Antagonist, Nutlin-3, Racemic (Cat. No. 444151) in DMSO is also available.
A cell-permeable, potent, and selective MDM2 antagonist (IC50 = 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b) that displays antitumor properties. Activates the p53 pathway by binding MDM2 in the p53-binding pocket and inhibiting the MDM2-p53 interaction. Shown to induce apoptosis in several cancer cell lines with wild-type p53 and in xenografted tumor mice.


Biochem/physiol Actions

Cell permeable: yes
Primary Target
MDM2
Product does not compete with ATP.
Reversible: no
Target IC50: 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b


Packaging

Packaged under inert gas


Preparation Note

Following reconstitution, aliquot, purge with inert gas, and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.


Other Notes

Thompson, T., et al. 2004. J. Biol. Chem.279, 53015.
Vassilev, L.T., et al. 2004. Science303, 844.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany


Disclaimer

Toxicity: Harmful (C)


技术参数 Specifications
Quality Segment100
assay≥98% (TLC and HPLC)
formsolid
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,protect from light
solubilityDMSO: 25 mg/mL,ethanol: 25 mg/mL
shipped inwet ice
storage temp.−20°C
SMILES stringClc1ccc(cc1)C2N(C(=NC2c5ccc(cc5)Cl)c4c(cc(cc4)OC)OC(C)C)C(=O)N3CCNC(=O)C3
InChI1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)
InChI keyBDUHCSBCVGXTJM-UHFFFAOYSA-N
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