Bomedemstat ditosylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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

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.

Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2V617F 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.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.

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.Animal Model:Mx-Jak2V617F miceDosage: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.

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Apoptosis

Apoptosis

Apoptosis | Histone Demethylase

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1990504-72-7

864.02

C42H50FN7O8S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (115.74 mM; 超声助溶 )

Cc1ccc(cc1)S(O)(=O)=O.Cc1ccc(cc1)S(O)(=O)=O.[H][C@]1(C[C@H]1NCCC[C@H](NC(=O)c1ccc(cc1)-n1ccnn1)C(=O)N1CCN(C)CC1)c1ccc(F)cc1

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(-20℃)

With Ice Pack

≥ 2 years