Description
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.
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |