GSK-4112 | 9663

GSK-4112 is a selective agonist for REV-ERBα (EC₅₀ = 0.4 μM). At 10 μM, GSK-4112 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. GSK-4112 is useful as a chemical tool to probe the function of REV-ERbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.

GSK-4112 is a selective agonist for REV-ERBα (EC₅₀ = 0.4 μM). At 10 μM, GSK-4112 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. GSK-4112 is useful as a chemical tool to probe the function of REV-ERbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.

9663 | GSK-4112 DataSheet

Alternate Name/Synonyms: 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate; SR 6452

Appearance: Off-white solid

Formulation: N/A

CAS Number: 1216744-19-2

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₈H₂₁ClN₂O₄S

Molecular Weight: 396.89

Cell-Permeable?: Yes

Purity: ≥98%

Solubilities: DMSO (~ 10 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A selective agonist for REV-ERBα

MDL Number: MFCD12912412

PubChem CID: 50905018

SMILES: CC(C)(C)OC(=O)CN(CC1=CC=C(C=C1)Cl)CC2=CC=C(S2)[N+](=O)[O-]

InChi: 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

InChi Key: WYSLOKHVFKLWOU-UHFFFAOYSA-N