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DC-05

  Cat. No.:  DC23977   Featured
Chemical Structure
890643-16-0
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More than 5000 active chemicals with high quality for research!
Field of application
DC-05 is a selective, non-nucleoside DNA methyltransferase DNMT1 inhibitor with IC50 of 10.3 uM, displays 3.6-fold selectivity over PRMT1 and >15-fold over DNMT3A, DNMT3B, G9a, SUV39H1, MLL1, SET7/9..
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 890643-16-0
Chemical Name: 9H-Carbazole-9-ethanol, α-[[[2-(1H-indol-3-yl)ethyl]amino]methyl]-
Synonyms: DC-05
SMILES: OC(CN1C2C=CC=CC=2C2C1=CC=CC=2)CNCCC1C2C=CC=CC=2NC=1
Formula: C25H25N3O
M.Wt: 383.4855
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
Description: DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
Target: DNMT1:1.09 μM (Kd) DNMT1:10.3 μM (IC50) PRMT1:37.1 μM (IC50)
In Vitro: 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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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