Molecular structure of GSK4112, CAS Number: 1216744-19-2
GSK4112 (CAS 1216744-19-2)
See product citations (1)
Alternate Names:
1,1-Dimethylethyl-N-[(4-chloropheny l)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate; GSK 4112
CAS Number:
1216744-19-2
Purity:
≥98%
Molecular Weight:
396.89
Molecular Formula:
C18H21ClN2O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Product Citations
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
GSK4112 is a reverb agonist. GSK4112 might provide insight into potential rythm disorders. Reverb-alpha 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. Reverb is negatively regulated by GSK3beta phosphorylation (among other things). GSK4112 competes with the heme (reverb natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. Reverb-alpha is a potential target for a small molecule drug to reset the cricadian clock. GSK4112 is an activator of Rev-erb alpha.
GSK4112 (CAS 1216744-19-2) References
- Ligand modulation of REV-ERBalpha function resets the peripheral circadian clock in a phasic manner. | Meng, QJ., et al. 2008. J Cell Sci. 121: 3629-35. PMID: 18946026
- GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. | Grant, D., et al. 2010. ACS Chem Biol. 5: 925-32. PMID: 20677822
- Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. | Kojetin, D., et al. 2011. ACS Chem Biol. 6: 131-4. PMID: 21043485
- A role for rev-erbα ligands in regulation of adipogenesis. | Kojetin, DJ. and Burris, TP. 2011. Curr Pharm Des. 17: 320-4. PMID: 21375499
- The nuclear receptor REV-ERBα mediates circadian regulation of innate immunity through selective regulation of inflammatory cytokines. | Gibbs, JE., et al. 2012. Proc Natl Acad Sci U S A. 109: 582-7. PMID: 22184247
- Rev-erbα regulates circadian rhythms and StAR expression in rat granulosa cells as identified by the agonist GSK4112. | Chen, H., et al. 2012. Biochem Biophys Res Commun. 420: 374-9. PMID: 22425774
- DBC1 (Deleted in Breast Cancer 1) modulates the stability and function of the nuclear receptor Rev-erbα. | Chini, CC., et al. 2013. Biochem J. 451: 453-61. PMID: 23398316
- Integration of the nuclear receptor REV-ERBα linked with circadian oscillators in the expressions of Alas1, Ppargc1a, and Il6 genes in rat granulosa cells. | Chen, H., et al. 2015. Chronobiol Int. 32: 739-49. PMID: 26102301
- Stimulation of nuclear receptor REV-ERBs regulates tumor necrosis factor-induced expression of proinflammatory molecules in C6 astroglial cells. | Morioka, N., et al. 2016. Biochem Biophys Res Commun. 469: 151-7. PMID: 26616049
- A validated ultra-performance liquid chromatography-tandem mass spectrometry method to identify the pharmacokinetics of SR8278 in normal and streptozotocin-induced diabetic rats. | Dong, D., et al. 2016. J Chromatogr B Analyt Technol Biomed Life Sci. 1020: 142-7. PMID: 27038650
- Pharmacological activation of REV-ERBα represses LPS-induced microglial activation through the NF-κB pathway. | Guo, DK., et al. 2019. Acta Pharmacol Sin. 40: 26-34. PMID: 29950615
- Radiotherapy induces responses of lung cancer to CTLA-4 blockade. | Formenti, SC., et al. 2018. Nat Med. 24: 1845-1851. PMID: 30397353
- Rev-erbα Inhibits Proliferation and Promotes Apoptosis of Preadipocytes through the Agonist GSK4112. | Chu, G., et al. 2019. Int J Mol Sci. 20: PMID: 31547330
- Nr1d1 affects autophagy in the skeletal muscles of juvenile Nile tilapia by regulating the rhythmic expression of autophagy-related genes. | Wu, P., et al. 2020. Fish Physiol Biochem. 46: 891-907. PMID: 32072342
- REV-ERBα Agonist GSK4112 attenuates Fas-induced Acute Hepatic Damage in Mice. | Shao, R., et al. 2021. Int J Med Sci. 18: 3831-3838. PMID: 34790059
Activator of:
Rev-erb alpha.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK4112, 5 mg | sc-300774 | 5 mg | $88.00 | |||
GSK4112, 10 mg | sc-300774A | 10 mg | $202.00 |