197345 BCL6 Inhibitor, 79-6 - Calbiochem

197345
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₉BrN₂O₆S₂

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197345-50MG
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      Glass bottle 50 mg
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      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®
      SynonymsCID5721353, 2-((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
      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
      SynonymsCID5721353, 2-((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
      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.