GSK 4112

Pricing Availability   Qty
Description: Selective Rev-Erbα agonist
Alternative Names: SR 6452
Chemical Name: 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate
Purity: ≥98% (HPLC)
Citations (4)

Biological Activity for GSK 4112

GSK 4112 is a selective Rev-Erbα agonist (EC50 = 250 nM). Enhances recruitment of nuclear receptor co-repressor (NCoR) peptide to Rev-Erbα; causes acute suppression of Bmal1 gene transcription. Induces phase shifts in the circadian clock.

Compound Libraries for GSK 4112

GSK 4112 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 4112

M. Wt 396.89
Formula C18H21ClN2O4S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1216744-19-2
PubChem ID 50905018
Smiles CC(C)(C)OC(CN(CC2=CC=C(Cl)C=C2)CC1=CC=C([N+]([O-])=O)S1)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GSK 4112

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 9.92 25

Preparing Stock Solutions for GSK 4112

The following data is based on the product molecular weight 396.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 10.08 mL 50.39 mL 100.78 mL
1.25 mM 2.02 mL 10.08 mL 20.16 mL
2.5 mM 1.01 mL 5.04 mL 10.08 mL
12.5 mM 0.2 mL 1.01 mL 2.02 mL

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References for GSK 4112

References are publications that support the biological activity of the product.

Meng et al (2008) Ligand modulation of REV-ERBα function resets the peripheral circadian clock in a phasic manner. J.Cell Science 121 3629 PMID: 18946026

Kojetin et al (2011) Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem.Biol. 6 131 PMID: 21043485

If you know of a relevant reference for GSK 4112, please let us know.

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Keywords: GSK 4112, GSK 4112 supplier, GSK4112, REV-ERBA, REV-ERBα, REV-ERBalpha, agonists, circadian, rhythms, SR6452, SR, 6452, Rev-Erb, Receptors, 3663, Tocris Bioscience

4 Citations for GSK 4112

Citations are publications that use Tocris products. Selected citations for GSK 4112 include:

Isaac Kirubakaran et al (2023) Circadian clock molecule REV-ERBα regulates lung fibrotic progression through collagen stabilization. Nat Commun 14 1295 PMID: 36894533

Chandra et al (2015) NR1D1 ameliorates Mycobacterium tuberculosis clearance through regulation of autophagy. Autophagy 11 1987 PMID: 26390081

Irfan et al (2021) Molecular clock REV-ERBα regulates cigarette smoke-induced pulmonary inflammation and epithelial-mesenchymal transition. JCI Insight 6 PMID: 34014841

Hyun Ok et al (2022) Sinapic Acid Ameliorates REV-ERB α Modulated Mitochondrial Fission against MPTP-Induced Parkinson's Disease Model. Biomol Ther (Seoul) 30 409-417 PMID: 35611585

Do you know of a great paper that uses GSK 4112 from Tocris? Please let us know.

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