Bomedemstat ditosylate

Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 ( LSD1 ) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis. In Vitro Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2 V617F cells by concomitantly increasing expression and methylation of p53. Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: SET-2 cells Concentration: 50 nM, 100 nM, and 1 μM Incubation Time: 96 hours Result: Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA. In Vivo Bomedemstat treatment (oral gavage; 45 mg/kg; once daily; 56 d) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mx-Jak2 V617F mice Dosage: 45 mg/kg Administration: Oral gavage; 45 mg/kg; once daily; 56 days Result: Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination. Form:Solid

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