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.