|3-(8-羟基喹啉-6-基)-N-(3-苯基丙基)苯甲酰胺|CsnPharm

CAS No.: 2003260-55-5

3-(8-Hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide Catalog No. CSN21075

Synonyms: KDM4B Inhibitor B3;KDM4B-IN-B3

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

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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^[1].
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.
参考文献

[1] Duan L, Rai G, Roggero C, Zhang QJ, Wei Q, Ma SH, Zhou Y, Santoyo J, Martinez ED, Xiao G, Raj GV, Jadhav A, Simeonov A, Maloney DJ, Rizo J, Hsieh JT, Liu ZP. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96. doi: 10.1016/j.chembiol.2015.08.007. Epub 2015 Sep 10. PMID: 26364928; PMCID: PMC4578295.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6147 mL
- 13.0735 mL
- 26.1469 mL
- 5 mM
- 0.5229 mL
- 2.6147 mL
- 5.2294 mL
- 10 mM
- 0.2615 mL
- 1.3073 mL
- 2.6147 mL

技术信息

CAS号

2003260-55-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H22N2O2

运输

蓝冰

分子量

382.45

别名

KDM4B Inhibitor B3;KDM4B-IN-B3

溶解度

DMSO	150.0 mg/mL (392.2 mM)
Water	insoluble

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3-(8-Hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide Catalog No. CSN21075

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