Bomedemstat (Synonyms: IMG-7289) |
| Catalog No.GC64865 |
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
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Cas No.: 1990504-34-1
Sample solution is provided at 25 µL, 10mM.
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Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1].
Bomedemstat (IMG-7289) selectively inhibits proliferation and induces apoptosis of JAK2V617F cells by concomitantly increasing expression and methylation of p53, and, independently, the pro-apoptotic factor PUMA and by decreasing the levels of its antiapoptotic antagonist BCL-XL[1]. Bomedemstat (25 nM, 50 nM) and Ruxolitinib (175 nM) synergize in inhibiting JAK2V617F-driven proliferation[1].Bomedemstat (50 and 100 nM) exerts a pro-apoptotic effect on 3 key regulators of programmed cell death, TP53, BCL-XL, and PUMA[1].
Once-daily treatment with Bomedemstat (IMG-7289; 45 mg/kg) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].
[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.
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