554718

REV-ERBα Antagonist, SR8278

The REV-ERBα Antagonist, SR8278 controls the biological activity of REV-ERBα.

• Synonym(e): REV-ERBα Antagonist, SR8278, SR8278SR 8278
• Empirische Formel (Hill-System): C₁₈H₁₉NO₃S₂
• CAS-Nummer: 101910-24-1
• Molekulargewicht: 361.48
• MDL number: MFCD00211150
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: >95% (HPLC)
• Form: gum, solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Segment: 100
• assay: >95% (HPLC)
• form: gum, solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white to yellow-brown
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: n1c2c(ccc1COc3cc(ccc3)C(O)CCCCC)cccc2
• InChI key: JRLOEMCOOZSCQP-UHFFFAOYSA-N

Beschreibung

General description

A cell-permeable REV-ERB antagonist that inhibits REV-ERBα transcriptional repression activity (EC₅₀ = 0.47 µM) in a REV-ERB target gene assay. It is also shown to block the ability of GSK4112 to enhance REV-ERB-&alpha-dependent repression (EC₅₀ = 0.35 µM) in a co-transfection assay. Treatment of HepG2 cells with SR8278 at 10 µM results in a significant increase in the expression of either G6Pase and PEPCK mRNA expression, consistent with its antagonistic role against endogenous heme.

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

Kojetin, D., et al. 2010, Chem Bio in press

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable