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GSK4112

Catalog No. T5045   CAS 1216744-19-2
Synonyms: 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate, SR6452

GSK4112 (SR6452) is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

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GSK4112 Chemical Structure
GSK4112, CAS 1216744-19-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 77.00
25 mg In stock $ 163.00
50 mg In stock $ 296.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK4112 (SR6452) is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.
Targets&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.
Synonyms 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate, SR6452
Molecular Weight 396.89
Formula C18H21ClN2O4S
CAS No. 1216744-19-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 9.9 mg/mL(25 mM)

TargetMolReferences and Literature

1. Grant D, et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol. 2010 Oct 15;5(10):925-932. 2. Xu L, yi Zhou W, Xu T, et al. Rev-erbα Mediates Steatosis in Alcoholic Fatty Liver Through Regulating Autophagy[J]. bioRxiv. 2021

TargetMolCitations

1. Xu L, yi Zhou W, Xu T, et al. Rev-erbα Mediates Steatosis in Alcoholic Fatty Liver Through Regulating Autophagy. Cell & Bioscience. 2021 Jul 10;11(1):129. doi: 10.1186/s13578-021-00622-4. 2. Liu Q, Xu L, Wu M, et al. Rev-erbα exacerbates hepatic steatosis in alcoholic liver diseases through regulating autophagy. Cell & Bioscience. 2021, 11(1): 1-15.

Related compound libraries

This product is contained In the following compound libraries:
Autophagy Compound Library Bioactive Compound Library Bioactive Compounds Library Max Nuclear Receptor Compound Library NO PAINS Compound Library Anti-Aging Compound Library

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Keywords

GSK4112 1216744-19-2 Autophagy hepatic damage HepG2 SR 6452 Apoptosis mice Inhibitor gluconeogenesis bmal1 HDAC 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate GSK-4112 hepatic gene probe SR-6452 Jo2 inhibit Fas SR6452 GSK 4112 transcription inhibitor

 

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