NCGC00247743 - Histone Demethylase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENCGC00247743Cat. No.: HY-112308CAS No.: 1435192-04-3分式: CHNO分量: 391.51作靶點(diǎn): Histone Demethylase作通路: Epigenetics儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 62.5 mg/mL (159.64 mM; Need ult

2、rasonic)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5542 mL 12.7711 mL 25.5421 mL5 mM 0.5108 mL 2.5542 mL 5.1084 mL10 mM 0.2554 mL 1.2771 mL 2.5542 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NCGC00247743種組蛋賴氨酸脫甲酶 KDM4 抑制劑。IC50 & Target KD

3、M4 1體外研究Based on structure-activity relationship studies, a series of chemical compounds are derived from 8-hydroxyquinoline (8HQ) and shown to be active inhibitors of KDM4E and KDM4A. The effect of these1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEcompounds is tested on the growth of LNCaP cell

4、s and NCGC00247751 (A1), NCGC00244536 (B3), andNCGC00247743 (I9) are selected. These inhibitors inhibit LNCaP cell growth with IC50s in the M range.These compounds also inhibit the enzymatic activity of other KDM4 isoforms although, interestingly, thepotency and efficacy of B3 and A1 for KDM4A, 4C,

5、and 4D are lower compared to that of NCGC00247743(I9), suggesting a potential selectivity of the inhibitors for different isoforms of KDM4 1.REFERENCES1. Duan L, et al. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR andBMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 0