GSK 4112
IC50: 2.3 μM
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.
Clinical trial: N/A
Reference:
[1] Daniel Grant,Lei Yin,Jon L. Collins et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear Heme receptor Rev-erbα. ACS CHEMICAL BIOLOGY5(10):925-32.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 396.89 |
| Cas No. | 1216744-19-2 |
| Formula | C18H21ClN2O4S |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥11.9 mg/mL in DMSO |
| Chemical Name | tert-butyl 2-((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)acetate |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC=C(CN(CC2=CC=C([N+]([O-])=O)S2)CC(OC(C)(C)C)=O)C=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
