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500655 Rad6 Inhibitor, TZ9 - CAS 1002789-86-7 - Calbiochem

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5.00655.0001
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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®
      Synonyms4-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, HHR6 Inhibitor, TZ9, TZ-9, TZ 9
      References
      ReferencesSanders, M.A., et al. 2013. Mol. Cancer Ther. 12, 373.
      Product Information
      CAS number1002789-86-7
      FormPale yellow solid
      Hill FormulaC₁₇H₁₄N₆O₄
      Chemical formulaC₁₇H₁₄N₆O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      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
      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
      Global Trade Item Number
      Référence GTIN
      5.00655.0001 04055977245059