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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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

500655
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Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
5.00655.0001 Glass bottle 10 mg
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
Catalogue Number GTIN
5.00655.0001 04055977245059

Documentation

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

Title

Safety Data Sheet (SDS) 

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