500017-70-9

500017-70-9 structure

Name: DC_517
Chemical Name: DC_517
CAS Number: 500017-70-9
Molecular Formula: C₃₃H₃₅N₃O₂
Molecular Weight: 505.650
Catalog: Signaling Pathways Epigenetics DNA Methyltransferase
Create Date: 2018-01-15 13:31:04
Modify Date: 2024-01-07 07:29:53
DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.

Name	DC_517
Synonyms	1-{[1,3-Di(9H-carbazol-9-yl)-2-propanyl]oxy}-3-(isopropylamino)-2-propanol 2-Propanol, 1-[2-(9H-carbazol-9-yl)-1-(9H-carbazol-9-ylmethyl)ethoxy]-3-[(1-methylethyl)amino]-

Description	DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.
Related Catalog	Signaling Pathways >> Epigenetics >> DNA Methyltransferase Research Areas >> Cancer
Target	DNMT1:0.91 μM (Kd) DNMT1:1.7 μM (IC50)
In Vitro	DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively. DC_517 (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. DC_517 (0, 0.75, 1.5, and 3 μM) also dose-dependently induces apoptotic cell death in HCT116 cells[1].
Kinase Assay	To measure the effects of DC_517 on mouse DNMT1 activity, 200 nM purified DNMT1 is incubated with 200 μM of DC_517 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].
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):9028-9041.