CAS:1401966-69-5GSK2879552

GSK2879552 is an irreversible inhibitor of lysine specific demethylase 1 (LSD1) with Ki of 1.7 μM with antineoplastic activity.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1401966-69-5

储存条件

分子式

C23H28N2O2

运输

蓝冰

分子量

364.48

别名

溶解度

DMSO	50.0 mg/mL (137.2 mM) warming

动物实验配方

生物活性

靶点 KDM1A

Ki:1.7μM
描述GSK2879552 is a potent, selective and irreversible LSD1 inhibitor. Inhibition of LSD1 by GSK2879552 increased the sensitivity of proliferation of a number of tumor types indicated that small cell lung carcinoma (SCLC), which was associated with DNA hypomethylation. Oral administration of GSK2879552 at dose of 1.5mg/kg inhibited tumor growth of subcutaneous NCI-H526 and NCI-H1417 xenografts by 57% and 83%. GSK2879552 increased H3K4 methylation selectively at genomic regions bound by LSD, resulting in gene expression changes across SCLC cell lines.
作用机制GSK2879552 can covalently bind to and form a complex with FAD and LSD1/CoREST.^[1]
动物研究
剂量
Mice: 1.5 mg/kg^[1] (p.o.), 33 mg/kg^[1] (i.p.)

给药途径
p.o., i.p.