CAS:2003260-55-5NCGC00244536

Synonyms: KDM4B Inhibitor B3

NCGC00244536 is a selective inhibitor of KDM4A with IC50 of 10 nM.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

2003260-55-5

储存条件

分子式

C25H22N2O2

运输

蓝冰

分子量

382.45

别名

KDM4B Inhibitor B3

溶解度

DMSO	150.0 mg/mL (392.2 mM)
Water	insoluble

动物实验配方

生物活性

描述Histone methylation is a key epigenetic marker involved in tumorigenesis. The overexpression of histone lysine demethylase KDM4 has been observed in multiple human cancer. NCGC00244536 is a novel, potent KDM4 inhibitor with an IC₅₀ value of 10 nM. It showed a high selective inhibitory effect on the fast-growing AR-negative PC3 cells with an IC₅₀ value of 40 nM. It potently inhibited AR-positive LNCaP and VCaP cell lines with IC₅₀ values less than 1 μM. It also impeded the growth of breast cancer cell lines MDA-MB2 and MCF-7 with IC₅₀ values in the micromolar range. Treatment of LNCaP and PC3 cells with 1 μM NCGC00244536 decreased the number of S phase cells. In SCID mice, daily treatment with 20 mg/kg NCGC00244536 significantly inhibited the tumor growth as compared to the vehicle-treated group without causing any major toxicity. Tumors harvested from NCGC00244536-treated mice showed a significant amount of cell necrosis, apoptosis, and fibrosis.
作用机制NCGC00244536 is a potent KDM4 inhibitor. It specifically binds to the domain of KDM4s, significantly suppressing the binding of KDM4B to the promoter or enhancer regions of target genes.