Molecular structure of GSK J1, CAS Number: 1373422-53-7
GSK J1 (CAS 1373422-53-7)
Alternate Names:
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Application:
GSK J1 is a selective and potent inhibitor of JMJDE and UTX demethylases
CAS Number:
1373422-53-7
Purity:
≥98%
Molecular Weight:
389.45
Molecular Formula:
C22H23N5O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GSK J1 is a selective and potent inhibitor of the H3K27 histone demethylases JMJDE and UTX. Suggested to display no activity against other JMJD family demethylases, and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 muM. This compound is a powerful and specific blocker of the histone demethylases JMJD3 and UTX, which are responsible for the removal of methyl groups from the H3K27 histone.
GSK J1 (CAS 1373422-53-7) References
- Inhibition of demethylases by GSK-J1/J4. | Heinemann, B., et al. 2014. Nature. 514: E1-2. PMID: 25279926
- Histone demethylase Utx regulates differentiation and mineralization in osteoblasts. | Yang, D., et al. 2015. J Cell Biochem. 116: 2628-36. PMID: 25920016
- Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors. | Hu, J., et al. 2016. Bioorg Med Chem Lett. 26: 721-725. PMID: 26776360
- Structural analysis of human KDM5B guides histone demethylase inhibitor development. | Johansson, C., et al. 2016. Nat Chem Biol. 12: 539-45. PMID: 27214403
- Small Molecule GSK-J1 Affects Differentiation of Specific Neuronal Subtypes in Developing Rat Retina. | Raeisossadati, R., et al. 2019. Mol Neurobiol. 56: 1972-1983. PMID: 29981055
- Inhibition of Ezh2 In Vitro and the Decline of Ezh2 in Developing Midbrain Promote Dopaminergic Neurons Differentiation Through Modifying H3K27me3. | Hong, F., et al. 2019. Stem Cells Dev. 28: 649-658. PMID: 30887911
- Sleep and Neurochemical Modulation by DZNep and GSK-J1: Potential Link With Histone Methylation Status. | Murillo-Rodríguez, E., et al. 2019. Front Neurosci. 13: 237. PMID: 30930741
- Screening of inhibitors against histone demethylation jumonji domain-containing protein 3 by capillary electrophoresis. | Zhang, Y., et al. 2020. J Chromatogr A. 1613: 460625. PMID: 31668999
- Early secreted antigenic target of 6-kDa of Mycobacterium tuberculosis induces transition of macrophages into epithelioid macrophages by downregulating iNOS / NO-mediated H3K27 trimethylation in macrophages. | Lin, J., et al. 2020. Mol Immunol. 117: 189-200. PMID: 31816492
- Therapeutically targeting head and neck squamous cell carcinoma through synergistic inhibition of LSD1 and JMJD3 by TCP and GSK-J1. | Zhang, W., et al. 2020. Br J Cancer. 122: 528-538. PMID: 31848446
- The JMJD3 histone demethylase inhibitor GSK-J1 ameliorates lipopolysaccharide-induced inflammation in a mastitis model. | Wang, JJ., et al. 2022. J Biol Chem. 298: 102017. PMID: 35526564
- EZH2 regulates the balance between osteoclast and osteoblast differentiation to inhibit arthritis-induced bone destruction. | Cheng, F., et al. 2022. Genes Immun. 23: 141-148. PMID: 35581496
- JMJD3/H3K27me3 epigenetic modification regulates Th17/Treg cell differentiation in ulcerative colitis. | Leng, XY., et al. 2022. Int Immunopharmacol. 110: 109000. PMID: 35777266
- GSK-J1-loaded, hyaluronic acid-decorated metal-organic frameworks for the treatment of ovarian cancer. | Yang, B., et al. 2022. Front Pharmacol. 13: 1023719. PMID: 36419626
Inhibitor of:
CRBP II, Histone cluster 1 H2AB, Histone cluster 1 H2AC, Histone cluster 1 H3D, Histone cluster 3 H2BB, Histone cluster 3 H3, JMJD1B, JMJD1C, JMJD2A, JMJD2B, JMJD3, JMJD4, JMJD7-PLA2G4B, JMJD8, MLLT (Mixed Lineage Leukemia Translocated), MSL-1, NSD3, OTTMUSG00000016784, PHF15, PHF8, PLU-1, SmcX, UTX, and ZSCAN4D.Activator of:
DDB1, Jumonji, PHF6, RGMb, SMYD3, UTY, and ZBTB43.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK J1, 10 mg | sc-391113 | 10 mg | $189.00 | |||
GSK J1, 50 mg | sc-391113A | 50 mg | $797.00 |