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.
性状
Solid
IC50 & Target[1][2]
KDM1/LSD1
体外研究(In Vitro)
Bomedemstat dihydrochloride 通过同时增加 p53 的表达和甲基化选择性抑制 Jak2 细胞增殖并诱导其凋亡。Bomedemstat (50 nM-1 μM; 96 h; SET-2 细胞) dihydrochloride 提高存活率,以 TP53 依赖性方式通过 BCL-XL 和 PUMA 诱导细胞凋亡,并导致细胞周期停滞。 has not independently confirmed the accuracy of these methods. They are for reference only.Apoptosis Analysis
体内研究(In Vivo)
Bomedemstat (oral gavage; 45?mg/kg; once daily; 56 d) dihydrochloride 可使血细胞计数正常化或改善血细胞计数,减少脾脏体积,恢复正常的脾脏结构,并减少骨髓纤维化。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Mx-Jak2 mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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.