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

Rad6 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.

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Synonyme: TZ9, TZ-9, TZ 9, HHR6 Inhibitor, 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

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500655
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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®
      SynonymsTZ9, TZ-9, TZ 9, HHR6 Inhibitor, 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
      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
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5.00655.0001 04055977245059

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

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

      TitelChargennummer
      500655

      Literatur

      Übersicht
      Sanders, M.A., et al. 2013. Mol. Cancer Ther. 12, 373.
      Datenblatt

      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
      SynonymsTZ9, TZ-9, TZ 9, HHR6 Inhibitor, 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
      CAS number1002789-86-7
      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.