GSK4112

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GSK4112

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Cat No: 11931

Biochemicals - Receptor Pharmacology

REV-ERBα is a nuclear hormone receptor with roles in circadian rhythm, adipogenesis, lipid metabolism, and inflammation. It binds porphoryin heme and in response to fluctuations in heme levels in cells it recruits corepressors such as NCoR and HDAC3 to...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl]-glycine, 1,1-dimethylethyl ester

Correlated keywords:

REV-ERB? nuclear hormone receptors circadian rhythm adipogenesis lipids metabolisms inflammation hemes NCoR HDAC3 transcriptional repression agonists gluconeogenesis GSK 4112 REVERB? inhibits inhibitors inhibiting bmal1 ovaries metabolism

Product Overview:
REV-ERBα is a nuclear hormone receptor with roles in circadian rhythm, adipogenesis, lipid metabolism, and inflammation. It binds porphoryin heme and in response to fluctuations in heme levels in cells it recruits corepressors such as NCoR and HDAC3 to repress the transcription of key genes involved in metabolic and circadian pathways.{21478,21474} GSK4112 is a synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that was designed to mimic the action of heme.{21476,21477} At 10 μM, GSK4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.{21476} GSK4112 has been used to investigate the function of REV-ERBα in the coordination of circadian rhythm and metabolism in rat ovaries.{21475}

Size	5 mg
Shipping	dry ice
CAS Number	1216744-19-2
Molecular Formula	C₁₈H₂₁ClN₂O₄S
SMILES	ClC(C=C1)=CC=C1CN(CC(OC(C)(C)C)=O)CC2=CC=C([N+]([O-])=O)S2
Molecular Weight	396,9
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO Guide 34:2009

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