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Merck
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G0673

Sigma-Aldrich

GSK4112

≥98% (HPLC)

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C18H21ClN2O4S
Numéro CAS:
1216744-19-2
Poids moléculaire :
396.89
Numéro MDL:
MFCD12912412
Code UNSPSC :
12352200
ID de substance PubChem :
329799818
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

off-white to tan

Solubilité

DMSO: >20 mg/mL

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne SMILES 

CC(C)(C)OC(=O)CN(Cc1ccc(Cl)cc1)Cc2ccc(s2)[N+]([O-])=O

InChI

1S/C18H21ClN2O4S/c1-18(2,3)25-17(22)12-20(10-13-4-6-14(19)7-5-13)11-15-8-9-16(26-15)21(23)24/h4-9H,10-12H2,1-3H3

Clé InChI

WYSLOKHVFKLWOU-UHFFFAOYSA-N

Actions biochimiques/physiologiques

GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba.

Caractéristiques et avantages

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictogrammes

Health hazardCorrosion
GHS08,GHS05

Mention d'avertissement

Danger

Mentions de danger

H318,H334

Classification des risques

Eye Dam. 1 - Resp. Sens. 1

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 1

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Norimitsu Morioka et al.
Brain, behavior, and immunity, 78, 116-130 (2019-01-27)
The orphan nuclear receptors REV-ERBα and REV-ERBβ (REV-ERBs) are crucial in the regulation of inflammatory-related gene transcription in astroglioma cells, but their role in nociceptive transduction has yet to be elaborated. Spinal dorsal horn astrocytes contribute to the maintenance of
Guiyan Chu et al.
International journal of molecular sciences, 20(18) (2019-09-25)
Proliferation and apoptosis are important physiological processes of preadipocytes. Rev-erbα is a circadian clock gene, and its activity contributes to several physiological processes in various cells. Previous studies demonstrated that Rev-erbα promotes preadipocyte differentiation, but a role of Rev-erbα on
Kayoko Ishimaru et al.
International journal of molecular sciences, 20(24) (2019-12-19)
The cell-autonomous circadian clock regulates IgE- and IL-33-mediated mast cell activation, both of which are key events in the development of allergic diseases. Accordingly, clock modifiers could be used to treat allergic diseases, as well as many other circadian-related diseases
Dong-Kai Guo et al.
Acta pharmacologica Sinica, 40(1), 26-34 (2018-06-29)
REV-ERBα, the NR1D1 (nuclear receptor subfamily 1, group D, member 1) gene product, is a dominant transcriptional silencer that represses the expression of genes involved in numerous physiological functions, including circadian rhythm, inflammation, and metabolism, and plays a crucial role
Na-Lee Ka et al.
Molecular and cellular endocrinology, 454, 87-92 (2017-06-11)
Cancer cells exhibit an elevated intracellular level of reactive oxygen species (ROS) because of their accelerated metabolism, mitochondrial dysfunction, and antioxidant deficit. The oxidative stress in cancer cells may provide clinical benefits, which can be associated with a better response
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