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.

• Synonim(y): REV-ERBα Agonist, GSK4112, GSK4112
• Wzór empiryczny (zapis Hilla): C₁₈H₂₁ClN₂O₄S
• Numer CAS: 1216744-19-2
• Masa cząsteczkowa: 396.89
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: dark beige
• rozpuszczalność: DMSO: 50 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 2
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable