DM-01

• CAT Number: I014943
• CAS Number: 2355280-00-9
• Molecular Formula: C23H24F3N3O2
• Molecular Weight: 431.45
• Purity: ≥95%
• Synonyms: N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1-[[4-(trifluoromethyl)phenyl]methyl]pyrrole-3-carboxamide
• InChI: InChI=1S/C23H24F3N3O2/c1-13-9-15(3)28-21(30)19(13)10-27-22(31)20-14(2)11-29(16(20)4)12-17-5-7-18(8-6-17)23(24,25)26/h5-9,11H,10,12H2,1-4H3,(H,27,31)(H,28,30)
• InChIKey: XHYKDXOCUIJBHL-UHFFFAOYSA-N
• SMILES: CC1=CC(=C(C(=O)N1)CNC(=O)C2=C(N(C=C2C)CC3=CC=C(C=C3)C(F)(F)F)C)C

DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors[1].
Knockdown EZH2 in A549 cells results in the decrease of cell sensitivity to DM-01 at 50 and 100 μM concentrations. DM-01 also shows comparable inhibitory activity for K562 cells with an IC50 value of 58.706 μΜ[1].
DM-01 (5 and 10 μM; 24 hours) strongly inhibits the activity of EZH2 and results in abolished H3K27me expression in K562 cells[1].
DM-01 (5 and 10 μM) also increases the transcription expression of DIRAS3 in a dose dependent manner, a tumor suppressor in downstream of EZH2[1].

Reference

[1]. Qifan Zhou, et al. Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents. New Journal of Chemistry. 10 Jan 2020.