DC-05

Names

[ Name ]:
DC-05

[Synonym ]:
9H-Carbazole-9-ethanol, α-[[[2-(1H-indol-3-yl)ethyl]amino]methyl]-
1-(9H-Carbazol-9-yl)-3-{[2-(1H-indol-3-yl)ethyl]amino}propan-2-ol
1-(9H-Carbazol-9-yl)-3-{[2-(1H-indol-3-yl)ethyl]amino}-2-propanol
MFCD08236399
DC-05

Biological Activity

[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.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> DNA Methyltransferase

Research Areas >> Cancer

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
667.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₅H₂₅N₃O

[ Molecular Weight ]:
383.486

[ Flash Point ]:
357.5±31.5 °C

[ Exact Mass ]:
383.199768

[ LogP ]:
5.41

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.672

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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