500655 Rad6 Inhibitor, TZ9 - Calbiochem

500655
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00655.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable triazine compound that directly targets human E2 Ubiquitin-conjugating enzyme Rad6B/HHR6B catalytic site via noncovalent interactions and effectively inhibits Rad6B-Ub thioester bond formation as well as subsequent substrate ubiquitination without affecting UbcH5B/UBE2D2-catalyzed BCA2 ubiquitination. Shown to inhibit the proliferation of high Rad6B-expressing MDA-MB-231 (IC50 = 6 µM in 72 h), but not the low Rad6B-expressing, non-transformed MCF10A, via G2/M arrest and apoptosis induction. Two known cellular Rad6 substrates, β-catenin and PCNA, are reported to be downregulated following 24 h inhibitor treatment in MDA-MB-231 cultures (0.5 to 5 µM).
          Catalogue Number500655
          Brand Family Calbiochem®
          SynonymsHHR6 Inhibitor, TZ9, TZ-9, TZ 9, 4-Amino-6-(phenylamino)-[1,3,5]triazin-2-yl)methyl-4-nitrobenzoate, (4-Amino-6-(phenylamino)-1,3,5-triazin-2-yl)methyl 4-nitrobenzoate
          References
          ReferencesSanders, M.A., et al. 2013. Mol. Cancer Ther. 12, 373.
          Product Information
          FormPale yellow solid
          Hill FormulaC₁₇H₁₄N₆O₄
          Chemical formulaC₁₇H₁₄N₆O₄
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          ApplicationRad6 Inhibitor, TZ9, CAS 002789-86-7, is a cell-permeable inhibitor of Rad6B-Ub thioester bond formation and subsequent substrate ubiquitination. Directly binds to the catalytic site of Rad6B/HHR6B.
          Biological Information
          Primary TargetRad6B/HHR6B
          Purity≥99% 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
          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) 

          Certificates of Analysis

          TitleLot Number
          500655

          References

          Reference overview
          Sanders, M.A., et al. 2013. Mol. Cancer Ther. 12, 373.
          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.

          Revision01-July-2013 JSW
          SynonymsHHR6 Inhibitor, TZ9, TZ-9, TZ 9, 4-Amino-6-(phenylamino)-[1,3,5]triazin-2-yl)methyl-4-nitrobenzoate, (4-Amino-6-(phenylamino)-1,3,5-triazin-2-yl)methyl 4-nitrobenzoate
          DescriptionA cell-permeable triazine compound that is reported to directly target human E2 Ubiquitin-conjugating enzyme Rad6B/HHR6B catalytic site via noncovalent interactions and effectively inhibit Rad6B-Ub thioester bond formation and subsequent Ub transfer to H2A (by 61%; 1 h 25 nM drug preincubation prior to 1 h H2A ubiquitination reactoin) without affecting UbcH5B/UBE2D2-catalyzed BCA2 ubiquitination. Shown to inhibit the proliferation of high Rad6B-expressing MDA-MB-231 (IC50 = 6 µM in 72 h by MTT assays; 96.3% inhibition of 24 h colony formation by 10 µM inhibitior) via G2/M arrest and apoptosis induction, while exhibiting little toxicity toward low Rad6B-expressing, non-transformed MCF10A (2% and 19% inhibition in 72 h by 10 and 50 µM inhibitor, respectively; by MTT assays). Two known cellular Rad6 substrates, β-catenin and PCNA, are shown to be downregulated following 24 h inhibitor treatment in a dose-dependent manner in MDA-MB-231 cultures (0.5 to 5 µM).
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₁₄N₆O₄
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          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
          ReferencesSanders, M.A., et al. 2013. Mol. Cancer Ther. 12, 373.