Bomedemstat dihydrochloride IMG-7289 dihydrochloride|西域试剂

Bomedemstat dihydrochloride IMG-7289 dihydrochloride,99.32%

产品编号：Bellancom-109169C| 分子式：C₂₈H₃₆Cl₂FN₇O₂| 分子量：592.54

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-109169C	￥3500.00	杭州北京（现货）
Bellancom-109169C	￥5800.00	杭州北京（现货）
Bellancom-109169C	￥11500.00	杭州北京（现货）

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Bomedemstat dihydrochloride IMG-7289 dihydrochloride

产品介绍

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

生物活性

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.

体外研究

Bomedemstat dihydrochloride 通过同时增加 p53 的表达和甲基化选择性抑制Jak2^V617F 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。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

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.

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。

西域 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.

体内研究

西域 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.

体内研究

西域 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.