Biochem/physiol Actions

Reversible: yes

Primary TargetSUMO E2-thioester complex

Cell permeable: yes

General description

A cell-permeable trihydroxyflavone compound that prevents the transfer of SUMO (Cat. Nos. 662037, 662039, and 662042) from the E2 thioester to the substrate without affecting SUMO-activating enzyme E1 (SAE-1/2; Cat. Nos. 662073 and 662074) 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 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.

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 (Cat. Nos. 662037, 662039, and 662042) from the E2 thioester to the substrate without affecting SUMO-activating enzyme E1 (SAE-1/2; Cat. Nos. 662073 and 662074) 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.

Legal Information

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

Other Notes

Kim, Y.S., et al. 2013. Chem. Biol.20, 604.Cotelle, N., et al. 1996. Free Radic. Biol. Med.20, 35.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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.

Warning

Toxicity: Standard Handling (A)