DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively. DC-05 shows less potent activities against DNMT3A, DNMT3B, G9a, SUV39H1, MLL1, SET7/9, and PRMT1 (IC50: >200, >200, >150, >150, >150, >150, 37.1 μM). DC-05 (1.25, 2.5, 5, and 10 μM) potently inhibits the proliferation of HCT116 (human colon cancer) and Capan-1 (human pancreatic adenocarcinoma cells) after treatment for 24, 48, and 72 h[1].
Kinase Assay
To measure the effects of DC-05 on mouse DNMT1 activity, 200 nM purified DNMT1 is incubated with 200 μM of DC-05 and S-adenosylmethionine (AdoMet) in the DNMT assay buffer in the assay plate at 37°C for 2 h. Next, every sample is incubated with the capture and detection antibody, followed by incubation with developer solution for 10 min at room temperature. The absorbance is measured at 450 nm using a microplate reader. S-Adenosylhomocysteine (AdoHcy) is used as a positive control[1].
Cell Assay
Animal Administration
References
[1]. Chen S, et al. Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening. J Med Chem. 2014 Nov 13;57(21):9028-41.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
