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197345 BCL6 Inhibitor, 79-6 - Calbiochem

197345
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₉BrN₂O₆S₂

Products

Catalogue NumberPackaging Qty/Pack
197345-50MG Glass bottle 50 mg
Description
OverviewA cell-permeable oxindole compound that selectively inhibits the transcriptional repression activity of BCL6 (by ~70% at 50 µM in 293T-based reporter assays), but not that of three other BTB/POZ (bric-a-brac tramtrack broad complex/Poxvirus zinc finger) family members, Kaiso, HIC1, and PLZF, by direct BCL6 binding (Kd = 138 µM) via the BTB domain and blocking corepressor BBD- (BCL6 binding domain) mediated BCL6 interaction (IC50 = 212 µM & Ki = 147 µM in competitive binding against SMRT-BBD peptide), resulting in upregulation of BCL6 target genes in BCL-dependent DLBCL (diffuse large B cell lymphoma), but not BCL-independent Toledo and OCI-Ly4 cell lines. Shown to exhibit antiproliferative activity against DLBCL cell lines (IC50 from 24 to 936 µM) as well as primary human DLBCL cells in vitro and suppress BCL-dependent tumor growth in mice (<40% of control tumor size on day 9; 50 mg/kg/day via i.p.) in vivo.
Catalogue Number197345
Brand Family Calbiochem®
Synonyms2-((5Z)-5-(5-Bromo-2-oxo-1H-indol-3-ylidene)-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl)butanedioic acid, B-Cell Lymphoma 6 Inhibitor, CID5721353
References
ReferencesCerchietti, L.C., et al. 2010. Cancer Cell 17, 400.
Product Information
FormDark red powder
Hill FormulaC₁₅H₉BrN₂O₆S₂
Chemical formulaC₁₅H₉BrN₂O₆S₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationBCL6 Inhibitor, 79-6, is a cell-permeable, selective inhibitor of the transcriptional repression activity of BCL6 (by ~70% at 50 µM in 293T-based reporter assays
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
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

BCL6 Inhibitor, 79-6 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

BCL6 Inhibitor, 79-6 - Calbiochem Certificates of Analysis

TitleLot Number
197345

References

Reference overview
Cerchietti, L.C., et al. 2010. Cancer Cell 17, 400.
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.

Revision14-November-2011 RFH
Synonyms2-((5Z)-5-(5-Bromo-2-oxo-1H-indol-3-ylidene)-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl)butanedioic acid, B-Cell Lymphoma 6 Inhibitor, CID5721353
DescriptionA cell-permeable oxindole compound that selectively inhibits the transcriptional repression activity of BCL6 (by ~70% at 50 µM in 293T-based reporter assays), but not that of three other BTB/POZ (bric-a-brac tramtrack broad complex/Poxvirus zinc finger) family members, Kaiso, HIC1, and PLZF, by direct BCL6 binding (Kd = 138 µM) via the BTB domain and blocking corepressor BBD- (BCL6 binding domain) mediated BCL6 interaction (IC50 = 212 µM & Ki = 147 µM in competitive binding against SMRT-BBD peptide), resulting in upregulation of BCL6 target genes in BCL-dependent DLBCL (diffuse large B cell lymphoma), but not BCL-independent Toledo and OCI-Ly4 cell lines. Shown to exhibit antiproliferative activity against DLBCL cell lines (IC50 from 24 to 936 µM) as well as primary human DLBCL cells in vitro and suppress BCL-dependent tumor growth in mice (<40% of control tumor size on day 9; 50 mg/kg/day via i.p.) in vivo.
FormDark red powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₅H₉BrN₂O₆S₂
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
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
ReferencesCerchietti, L.C., et al. 2010. Cancer Cell 17, 400.