GSK4112

SKU: orb1226777

Description

A potent and selective small molecule Rev-erbα agonist with EC50 of 0.4 uM in biochemical assay; mediates the repression of Rev-erbα target gene bmal1 in liver cells, and inhibits and shifts the phase of gluconeogenesis in primary mouse hepatocytes.

Key Properties

• CAS Number: 1216744-19-2
• MW: 396.8883
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₁ClN₂O₄S
• SMILES: O=C(OC(C)(C)C)CN(CC1=CC=C(Cl)C=C1)CC2=CC=C([N+]([O-])=O)S2
• Target: Autophagy
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage. Animal model: Male C57BL/6 mice with Fas-induced acute hepatic damage. Dosage: 25 mg/kg. Administration: Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure. Result: Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis.
• In Vitro:
  GSK4112 (0-100 μM; 1 h) interacts with Rev-erbα with an EC50 value of 0.4 μM. GSK4112 (10 μM; 6 h) represses expression of bmal1 and the target genes associated with the pathway of gluconeogenesis, recruits HDAC3 and modulates the effect of Rev-erbα on oscillation of hepatic gene expression. GSK4112 (10 μM; 16 h) reduces glucose output in murine hepatocytes. RT-PCR Cell line: HepG2 cell line. Concentration: 10 μM. Incubation time: 6 hours. Result: Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SR6452 | GSK-4112 | GSK 4112 | SR-6452 | SR 6452

Quick Database Links

Gene Symbol

Autophagy