BomedemSTAT (IMG-7289) hydrochloride 是一种具有口服活性和不可逆的lysine-specific demethylase 1(LSD1) 抑制剂。BomedemSTAT hydrochloride 可以增加 H3K4 和 H3K9 的甲基化，然后改变基因表达。BomedemSTAT hydrochloride 具有抗癌活性，可抑制癌细胞增殖并诱导细胞凋亡。

Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 ( LSD1 ) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] [2].

Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2 V617F cells by concomitantly increasing expression and methylation of p53 [1]. 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 [1]. Apoptosis Analysis [1] Cell 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.

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 [1]. Animal Model: Mx-Jak2 V617F mice [1] 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.

C28H35ClFN7O2

556.07

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years