GSK-J4 (Free base)

• CAT Number: I001438
• CAS Number: 1373423-53-0
• Molecular Formula: C₂₄H₂₇N₅O₂
• Molecular Weight: 417.50
• Purity: ≥95%
• Synonyms: ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
• Target: Histone Demethylases
• Solubility: DMSO: ≥ 42 mg/mL
• Storage: Store at -20°C
• IC50: 9 uM(TNF-a blockade)
• InChI: InChI=1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28)
• InChIKey: WBKCKEHGXNWYMO-UHFFFAOYSA-N
• SMILES: CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3

GSK-J4（Cat No.:I001438） is a potent inhibitor of H3K27me3/me2 demethylases, specifically targeting JMJD3/KDM6B and UTX/KDM6A with IC50 values of 8.6 μM and 6.6 μM, respectively. It effectively inhibits the production of TNF-α in human primary macrophages induced by LPS, with an IC50 of 9 μM. GSK-J4 is a prodrug of GSK-J1 and can penetrate cells. It induces apoptosis associated with endoplasmic reticulum stress. This compound holds potential for epigenetic research and modulation of inflammatory responses and apoptosis pathways.

Reference

[1]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.