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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-NCGC00244536
NCGC00244536

Chemical Structure : NCGC00244536

CAS No.: 2003260-55-5

NCGC00244536 (KDM4B Inhibitor B3)

货号: PC-26937Not For Human Use, Lab Use Only.

NCGC00244536 (B3) is a potent, speciifc lysine demethylase 4B (KDM4B, JMJD2B) inhibitor with an IC50 of 10 nM, inhibits LNCaP cell growth with IC50s in the μM range, shows no or weak activity for KDM5A/JARID1A.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NCGC00244536 (B3) is a potent, speciifc lysine demethylase 4B (KDM4B, JMJD2B) inhibitor with an IC50 of 10 nM, inhibits LNCaP cell growth with IC50s in the μM range, shows no or weak activity for KDM5A/JARID1A.
NCGC00244536 (B3) displays much weaker acitvities against KDM4A, 4C, and 4D.
NCGC00244536 (B3) displays high selectivity for the fast-growing AR-negative PC3 cells (IC50 40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4.
NCGC00244536 (B3) effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolar range.
NCGC00244536 (B3) is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC50s.
NCGC00244536 (B3) (20 mg/kg) induces significant inhibition of tumor growth in xenograft model with tumors derived from injection of PC3 cells.

物理化学性质&存储条件

分子量 382.46
分子式 C25H22N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(8-Hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide

参考文献

1. Duan L, et al. Chem Biol. 2015 Sep 17;22(9):1185-96.

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