5.05156

SUMOylation Inhibitor III, 2-D08

• Synonyme(s) : SUMOylation Inhibitor III, 2-D08, 2-(2,3,4-Trihydroxyphenyl)-4H-chromen-4-one, 2D08, SUMO E2 Ubc9 Inhibitor
• Formule empirique (notation de Hill): C₁₅H₁₀O₅
• Poids moléculaire : 270.24
• Code UNSPSC : 41100000
• Nomenclature NACRES : NA.24

Propriétés

• Pureté: ≥95% (HPLC)
• Niveau de qualité: 300
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: orange-brown
• Solubilité: DMSO: 25 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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.

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
SUMO E2-thioester complex

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

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.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable