505156 | SUMOylation Inhibitor III, 2-D08 - Calbiochem

505156
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₀O₅

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05156.0001
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          Glass bottle 10 mg
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          Description
          OverviewA 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.
          Catalogue Number505156
          Brand Family Calbiochem®
          Synonyms2-(2,3,4-Trihydroxyphenyl)-4H-chromen-4-one, 2D08, SUMO E2 Ubc9 Inhibitor
          References
          ReferencesKim, Y.S., et al. 2013. Chem. Biol. 20, 604.
          Cotelle, N., et al. 1996. Free Radic. Biol. Med. 20, 35.
          Product Information
          FormOrange-brown powder
          Hill FormulaC₁₅H₁₀O₅
          Chemical formulaC₁₅H₁₀O₅
          ReversibleY
          Applications
          Biological Information
          Primary TargetSUMO E2-thioester complex
          Purity≥95% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

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

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision18-April-2014 JSW
          Synonyms2-(2,3,4-Trihydroxyphenyl)-4H-chromen-4-one, 2D08, SUMO E2 Ubc9 Inhibitor
          DescriptionA 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.
          FormOrange-brown powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₅H₁₀O₅
          Purity≥95% by HPLC
          SolubilityDMSO (25 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesKim, Y.S., et al. 2013. Chem. Biol. 20, 604.
          Cotelle, N., et al. 1996. Free Radic. Biol. Med. 20, 35.