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GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 of 0.4 μM and serves as a small molecule chemical probe for studying the cell biology of the nuclear heme receptor Rev-erbα.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $46 | In Stock | |
25 mg | $98 | In Stock | |
50 mg | $178 | In Stock | |
100 mg | $319 | In Stock | |
200 mg | $459 | In Stock | |
1 mL x 10 mM (in DMSO) | $30 | In Stock |
Description | GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 of 0.4 μM and serves as a small molecule chemical probe for studying 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. |
Alias | SR6452, 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate |
Molecular Weight | 396.89 |
Formula | C18H21ClN2O4S |
Cas No. | 1216744-19-2 |
Smiles | CC(C)(C)OC(=O)CN(Cc1ccc(s1)[N+]([O-])=O)Cc1ccc(Cl)cc1 |
Relative Density. | 1.296 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 9.9 mg/mL (25 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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