REV-ERBα Agonist, GSK4112-Calbiochem

C₁₈H₂₁ClN₂O₄S

396.89

A 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.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Grant, D., et al. 2010, ACS Chem. Biol.5, 925.
Meng, Q., et al. 2008. Journ. Cell. Sci121, 3629.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

dark beige

DMSO: 50 mg/mL

ambient

−20℃

10 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 2