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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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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1216744-19-2C₁₈H₂₁ClN₂O₄S

Products

Catalogue NumberPackaging Qty/Pack
554716-10MGCN Glass bottle 10 mg
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.