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1216744-19-2

1216744-19-2 structure
1216744-19-2 structure
  • Name: GSK4112
  • Chemical Name: gsk 4112
  • CAS Number: 1216744-19-2
  • Molecular Formula: C18H21ClN2O4S
  • Molecular Weight: 396.888
  • Catalog: Signaling Pathways Autophagy Autophagy
  • Create Date: 2016-03-05 08:15:10
  • Modify Date: 2024-01-04 19:10:02
  • GSK4112 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.IC50 value: 0.4 μM (EC50)Target: Rev-erbαin 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.

Name gsk 4112
Synonyms 2-Methyl-2-propanyl N-(4-chlorobenzyl)-N-[(5-nitro-2-thienyl)methyl]glycinate
Glycine, N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl]-, 1,1-dimethylethyl ester
tert-Butyl N-(4-chlorobenzyl)-N-[(5-nitro-2-thienyl)methyl]glycinate
GSK4112
Description GSK4112 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.IC50 value: 0.4 μM (EC50)Target: Rev-erbαin 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.
Related Catalog
References

[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.

Density 1.3±0.1 g/cm3
Boiling Point 486.7±45.0 °C at 760 mmHg
Molecular Formula C18H21ClN2O4S
Molecular Weight 396.888
Flash Point 248.1±28.7 °C
Exact Mass 396.091064
PSA 103.60000
LogP 5.47
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.591
Storage condition 2-8℃
Precursor  4

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