DC-517-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDC_517Cat. No.: HY-12747CAS No.: 500017-70-9分式: CHNO分量: 505.65作靶点: DNA Methyltransferase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 : 50 mg/mL (98.88 mM)H2O : 40% PEG300 5

2、% Tween-80 45% salineSolubility: 3.25 mg/mL (6.43 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.25 mg/mL (6.43 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 3.25 mg/mL (6.43

3、mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DC_517种 DNMT1 抑制剂，IC50 和 Kd 值分别为 1.7 M 和 0.91 M。IC50 & Target DNMT1 DNMT10.91 M (Kd) 1.7 M (IC50)体外研究 DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 M and 0.91 M,respectively. DC_517 (1.25, 2.5, 5, and 10 M) potently inhi

4、bits the proliferation of HCT116 (human coloncancer) and Capan-1 (human pancreatic adenocarcinoma cells) after treatment for 24, 48, and 72 h. DC_517(0, 0.75, 1.5, and 3 M) also dose-dependently induces apoptotic cell death in HCT116 cells 1.PROTOCOLKinase Assay 1 To measure the effects of DC_517 on

5、 mouse DNMT1 activity, 200 nM purified DNMT1 is incubated with 200M of DC_517 and S-adenosylmethionine (AdoMet) in the DNMT assay buffer in the assay plate at 37C for2 h. Next, every sample is incubated with the capture and detection antibody, followed by incubation withdeveloper solution for 10 min

6、 at room temperature. The absorbance is measured at 450 nm using amicroplate reader. S-Adenosylhomocysteine (AdoHcy) is used as a positive control 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chen S, et al. Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. JMed Chem. 2014 Nov 13;57(21):9028-9041.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.