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5.05156 Millipore

SUMOylation Inhibitor III, 2-D08 - Calbiochem

Synonym: 2-(2,3,4-Trihydroxyphenyl)-4H-chromen-4-one, 2D08, SUMO E2 Ubc9 Inhibitor, SUMOylation Inhibitor III, 2-D08 - Calbiochem

  • Empirical Formula (Hill Notation) C15H10O5

  • Molecular Weight 270.24

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Properties

Related Categories Molecular Biology, Post-Translational Modification, Proteomics, Ubiquitination Analysis
Quality Level   300
assay   ≥95% (HPLC)
form   powder
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   orange-brown
solubility   DMSO: 25 mg/mL

Description

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 (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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
SUMO E2-thioester complex

Reversible: yes

Packaging

Packaged under inert gas

Warning

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.

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

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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