For research use only. Not for therapeutic Use.
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis[1][2].
Bomedemstat dihydrochloride selectively inhibits proliferation and induces apoptosis of Jak2V617F cells by concomitantly increasing expression and methylation of p53[1].
Bomedemstat (50 nM-1 μM; 96 h; SET-2 cells) dihydrochloride enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest[1].
Bomedemstat (oral gavage; 45 mg/kg; once daily; 56 d) dihydrochloride normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].
| Catalog Number | I041434 |
| Synonyms | N-[(2S)-5-[[(1R,2S)-2-(4-fluorophenyl)cyclopropyl]amino]-1-(4-methylpiperazin-1-yl)-1-oxopentan-2-yl]-4-(triazol-1-yl)benzamide;dihydrochloride |
| Molecular Formula | C28H36Cl2FN7O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H34FN7O2.2ClH/c1-34-15-17-35(18-16-34)28(38)25(3-2-12-30-26-19-24(26)20-4-8-22(29)9-5-20)32-27(37)21-6-10-23(11-7-21)36-14-13-31-33-36;;/h4-11,13-14,24-26,30H,2-3,12,15-19H2,1H3,(H,32,37);2*1H/t24-,25-,26+;;/m0../s1 |
| InChIKey | PPKDUCDLYRHGFX-DVNXTAPYSA-N |
| SMILES | CN1CCN(CC1)C(=O)C(CCCNC2CC2C3=CC=C(C=C3)F)NC(=O)C4=CC=C(C=C4)N5C=CN=N5.Cl.Cl |
| Reference | [1]. Jonas S Jutzi, et al. LSD1 Inhibition Prolongs Survival in Mouse Models of MPN by Selectively Targeting the Disease Clone. Hemasphere. 2018 Jun 8;2(3):e54. [2]. Yuan Fang, et al. LSD1/KDM1A inhibitors in clinical trials: advances and prospects. J Hematol Oncol. 2019 Dec 4;12(1):129. |
