554716

REV-ERBα Agonist, GSK4112

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

• Sinonimo/i: REV-ERBα Agonist, GSK4112, GSK4112
• Formula empirica (notazione di Hill): C₁₈H₂₁ClN₂O₄S
• Numero CAS: 1216744-19-2
• Peso molecolare: 396.89
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: dark beige
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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.

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable