GSK4112

SKU: orb1302143

Description

GSK4112 (SR6452) is a potent and selective synthetic agonist of the nuclear receptor Rev-erbα, demonstrating an EC50 of 0.4 μM. This chemical probe is widely used in vitro and in vivo to investigate circadian rhythm regulation, metabolic pathways, and inflammatory responses linked to Rev-erbα biology.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 1216744-19-2
• MW: 396.89
• Purity: 99.63%
• Formula: C₁₈H₂₁ClN₂O₄S
• SMILES: CC(C)(C)OC(=O)CN(Cc1ccc(s1)[N+]([O-])=O)Cc1ccc(Cl)cc1
• Target: Autophagy,REV-ERB,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.52 mM);DMSO:9.9 mg/mL (24.94 mM)

Bioactivity

• Target IC50:
  Rev-Erbα:0.4 μM(EC50)
• In Vitro:
  GSK4112 profiled as a Rev-erb agonist in cells to inhibit expression of the circadian target gene bmal1. In addition, GSK4112 repressed the expression of gluconeogenic genes in liver cells and reduced glucose output in primary hepatocytes. Therefore, GSK4112 is useful as a chemical tool to probe the function of Rev-erb in transcriptional repression, regulation of circadian biology, and metabolic pathways. Additionally, GSK4112 may serve as a starting point for design of Rev-erb chemical probes with in vivo pharmacologicalm activity.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

transcription, SR6452, SR-6452, SR 6452, Rev-ErbBα, probe, Autophagy, Apoptosis, bmal1, 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate, hepatic damage, hepatic gene, HepG2, HDAC, gluconeogenesis, GSK 4112, GSK-4112, GSK4112, Fas, Inhibitor, Jo2, inhibit, mice

Compound Identifiers

PubChem CID

50905018