Hdm2 E3 ligase inhibitor 1
Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase) -mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy[1].
Product Specifications
CAS Number
[414905-09-2]
UNSPSC
12352005
Target
E1/E2/E3 Enzyme; MDM-2/p53
Type
Reference compound
Related Pathways
Apoptosis; Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/hdm2-e3-ligase-inhibitor-1.html
Smiles
O=C(NC1=CC=C(S(=O)(N)=O)C=C1)C(C(F)(F)F)C(F)(F)F
Molecular Formula
C10H8F6N2O3S
Molecular Weight
350.24
References & Citations
[1]Lai Z, et al., Differentiation of Hdm2-mediated p53 ubiquitination and Hdm2 autoubiquitination activity by small molecular weight inhibitors. Proc Natl Acad Sci U S A. 2002 Nov 12;99 (23) :14734-9.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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