373225
Hdm2 E3 Ligase Inhibitor - CAS 414905-09-2 - Calbiochem
The Hdm2 E3 Ligase Inhibitor, also referenced under CAS 414905-09-2, controls the biological activity of Hdm2 E3 Ligase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
别名:
Hdm2 E3 Ligase Inhibitor - CAS 414905-09-2 - Calbiochem, N-((3,3,3-Trifluoro-2-trifluromethyl)propionyl)sulfanilamide, Mdm2 E3 Ligase Inhibitor, MDM2 Inhibitor V
assay
≥95% (NMR)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 50 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable and reversible inhibitor of Hdm2 E3 ligase that selectively blocks Hdm2 E3-mediated ubiquitination. Has been shown to inhibit ubiquitination of p53 in vitro (IC50 = 12.7 µM using Ub-Ubc as the donor substrate). Exhibits little effect towards other ubiquitin-using enzymes (IC50 >100 µM for E1, Nedd-4, and SCF) or the auto-ubiquitination activity of Hdm2. The inhibition is non-competitive with respect to either the donor or acceptor substrate.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
ubiquitination of p53 in vitro
ubiquitination of p53 in vitro
Product does not compete with ATP.
Reversible: yes
Target IC50: 12.7 µM inhibiting ubiquitination of p53 in vitro using Ub-Ubc as the donor substrate
Packaging
Packaged under inert gas
Other Notes
Lai, Z., et al. 2002. Proc. Natl. Acad. Sci. USA99, 14734.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
10-13 - German Storage Class 10 to 13
Zhihong Lai et al.
Proceedings of the National Academy of Sciences of the United States of America, 99(23), 14734-14739 (2002-10-31)
The oncoprotein hdm2 ubiquitinates p53, resulting in the rapid degradation of p53 through the ubiquitin (Ub)-proteasome pathway. Hdm2-mediated destabilization and inactivation of p53 are thought to play a critical role in a number of human cancers. We have used an
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