GSK4112 是一种 Rev-erbα 激动剂，EC50 为 0.4 μM。它也是一种用于核血红素受体 Rev-erbα 的细胞生物学的小分子化学探针。

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.

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.

1216744-19-2

C18H21ClN2O4S

396.89

1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate;SR6452;GSK4112

DMSO:9.9 mg/mL(25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years