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.

• 동의어(들): REV-ERBα Agonist, GSK4112, GSK4112
• 실험식(Hill 표기법): C₁₈H₂₁ClN₂O₄S
• CAS Number: 1216744-19-2
• Molecular Weight: 396.89
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: dark beige
• solubility: DMSO: 50 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C

설명

일반 설명

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.

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable