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554716 REV-ERBα Agonist, GSK4112 - CAS 1216744-19-2 - Calbiochem

The REV-ERBα Agonist, GSK4112 controls the biological activity of REV-ERBα. This small molecule/inhibitor is primarily used for Biochemicals applications.

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

Synonyms: GSK4112

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554716
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1216744-19-2C₁₈H₂₁ClN₂O₄S

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554716-10MGCN
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      Description
      OverviewA selective, cell-permeable ligand (EC50 = 250 nM) that acts as a REV-ERBα agonist using a FRET assay. It enhances the recruitment of NCoR peptide to REV-ERBα by up to 70%, and displays no activity towards LRH1, SF1, FXR or ROR, and LXR. Furthermore, it inhibits the promoter activity of Pai1, a known target for REV-ERBα by 30%. This ligand exhibits acute suppression of Bmal1 transcription, and is capable of resetting the molecular rhythm of REV-ERBα-mediated PER2 expression in both Rat-1 lung fibroblasts and on ectopic lung tissues in Luciferase reporter assays. In addition, it is shown to repress the expression of gluconeogenic genes in liver cells and reduce glucose output in primary hepatocytes.
      Catalogue Number554716
      Brand Family Calbiochem®
      SynonymsGSK4112
      References
      ReferencesGrant, D., et al. 2010, ACS Chem. Biol. 5, 925.
      Meng, Q., et al. 2008. Journ. Cell. Sci 121, 3629.
      Product Information
      CAS number1216744-19-2
      FormDark beige solid
      Hill FormulaC₁₈H₂₁ClN₂O₄S
      Chemical formulaC₁₈H₂₁ClN₂O₄S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      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 with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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
      Global Trade Item Number
      Catalogue Number GTIN
      554716-10MGCN 04055977193091

      Documentation

      REV-ERBα Agonist, GSK4112 - CAS 1216744-19-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      REV-ERBα Agonist, GSK4112 - CAS 1216744-19-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      554716

      References

      Reference overview
      Grant, D., et al. 2010, ACS Chem. Biol. 5, 925.
      Meng, Q., et al. 2008. Journ. Cell. Sci 121, 3629.
      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.

      Revision21-November-2011 RFH
      SynonymsGSK4112
      DescriptionA selective, cell-permeable ligand (EC50 = 250 nM) that acts as a REV-ERBα agonist using a FRET assay. It enhances the recruitment of NCoR peptide to REV-ERBα by up to 70%, and displays no activity towards LRH1, SF1, FXR or ROR, and LXR. Furthermore, it inhibits the promoter activity of Pai1, a known target for REV-ERBα by 30%. This ligand exhibits acute suppression of Bmal1 transcription, and is capable of resetting the molecular rhythm of REV-ERBα-mediated PER2 expression in both Rat-1 lung fibroblasts and on ectopic lung tissues in Luciferase reporter assays. In addition, it is shown to repress the expression of gluconeogenic genes in liver cells and reduce glucose output in primary hepatocytes.
      FormDark beige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1216744-19-2
      Chemical formulaC₁₈H₂₁ClN₂O₄S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesGrant, D., et al. 2010, ACS Chem. Biol. 5, 925.
      Meng, Q., et al. 2008. Journ. Cell. Sci 121, 3629.