EI1

• CAT Number: I001607
• CAS Number: 1418308-27-6
• Molecular Formula: C23H26N4O2
• Molecular Weight: 390.50
• Purity: ≥95%
• Synonyms: 6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
• Target: EZH2
• Solubility: 10 mM in DMSO
• Storage: Store at -20℃
• IC50: 15±2 nM (EZH2 wild type); 13±3 nM (EZH2 Y641F mutant type) [1]
• InChI: InChI=1S/C23H26N4O2/c1-5-17(6-2)27-8-7-18-19(10-16(12-24)11-21(18)27)22(28)25-13-20-14(3)9-15(4)26-23(20)29/h7-11,17H,5-6,13H2,1-4H3,(H,25,28)(H,26,29)
• InChIKey: PFHDWRIVDDIFRP-UHFFFAOYSA-N
• SMILES: CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C

EI1（Cat No.:I001607）is a selective inhibitor of the enzyme lysine-specific demethylase 1 (LSD1), which plays a critical role in the regulation of gene expression through histone methylation. By inhibiting LSD1, EI1 alters the epigenetic landscape of cancer cells, leading to reactivation of tumor suppressor genes and reduced cell proliferation. This compound has shown potential in preclinical studies, particularly in treating hematological malignancies and solid tumors associated with dysregulated LSD1 activity. EI1’s ability to modulate epigenetic regulation offers promising insights into developing targeted therapies for various cancers.

Reference

[1]. Qi W, et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5.