UNC0224

• CAT Number: I000722
• CAS Number: 1197196-48-7
• Molecular Formula: C26H43N7O2
• Molecular Weight: 485.70
• Purity: ≥95%
• Synonyms: 7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
• Target: Histone Methyltransferase
• Solubility: 10 mM in DMSO
• Storage: Store at 4°C
• IC50: 15 nM [1]
• InChI: InChI=1S/C26H43N7O2/c1-30(2)10-7-17-35-24-19-22-21(18-23(24)34-5)25(27-20-8-13-32(4)14-9-20)29-26(28-22)33-12-6-11-31(3)15-16-33/h18-20H,6-17H2,1-5H3,(H,27,28,29)
• InChIKey: XIVUGRBSBIXXJE-UHFFFAOYSA-N
• SMILES: CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C)OC)OCCCN(C)C

UNC0224(Cat No.:I000722) stands as a potent and selective inhibitor of the G9a enzyme, a key player in epigenetic regulation. With an impressive IC50 of 15 nM in the G9a Thioglo assay, UNC0224 demonstrates its capability to modulate the activity of G9a, a histone methyltransferase that contributes to gene expression and chromatin organization. By selectively targeting G9a, UNC0224 offers a valuable tool for investigating the intricate landscape of epigenetic modifications, potentially leading to novel therapeutic strategies for various diseases, including those rooted in aberrant gene regulation.

Reference

[1]. Liu F, et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem. 2009 Dec 24;52(24):7950-3.
[2]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57.