Merck, 5051560001, SUMOylation Inhibitor III, 2-D08

General description
A cell-permeable trihydroxyflavone compound that inhibits androgen receptor peptide, IκBα, and Topoisomerase I SUMOylation in cell-free assays (>90% at 30 µM) by selectively preventing the transfer of SUMO from the E2 thioester to the substrate without affecting SUMO-activating enzyme E1 or E2 Ubc9-SUMO thioester formation. A 6 h pretreatment with 100 µM 2-D08 is shown to effectively inhibit 10 µM CPT- (Camptothecin; Cat. No. 208925) induced cellular Topoisomerase I SUMOylation in breast cancer ZR-75-1 and BT-474 cultures without affecting overall cellular protein ubiquitinations. Anacardic and Ginkgolic Acid (Cat. No. 172050 and 345887, respectively) in comparison, both inhibit E1- SUMO thioester formation instead.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
SUMO E2-thioester complex
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.
Other Notes
Kim, Y.S., et al. 2013. Chem. Biol.20, 604.
Cotelle, N., et al. 1996. Free Radic. Biol. Med.20, 35.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)