5.05156
SUMOylation Inhibitor III, 2-D08
Synonym(s):
SUMOylation Inhibitor III, 2-D08, 2-(2,3,4-Trihydroxyphenyl)-4H-chromen-4-one, 2D08, SUMO E2 Ubc9 Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C15H10O5
Molecular Weight:
270.24
NACRES:
NA.24
UNSPSC Code:
41100000
assay
≥95% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange-brown
solubility
DMSO: 25 mg/mL
storage temp.
2-8°C
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
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.
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)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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