NCGC00247743 - Histone Demethylase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENCGC00247743Cat. No.: HY-112308CAS No.: 1435192-04-3分式: CHNO分量: 391.51作靶点: Histone Demethylase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 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制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NCGC00247743种组蛋赖氨酸脱甲酶 KDM4 抑制剂。IC50 & Target KD

3、M4 1体外研究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 您边的抑制剂师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