Bomedemstat (Synonyms: IMG-7289) |
| Catalog No.GC64865 |
Bomedemstat (IMG-7289) est un inhibiteur de la déméthylase spécifique de la lysine 1 (LSD1) actif par voie orale et irréversible. Bomedemstat peut augmenter la méthylation de H3K4 et H3K9, puis modifier l'expression des gènes. Bomedemstat présente des activités anticancéreuses, inhibe la prolifération des cellules cancéreuses et induit l'apoptose.
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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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