| Name | DC_05 |
|---|---|
| Synonyms |
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 |
| 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 | |
| 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 |
| 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 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302 |
| Precautionary Statements | P301 + P312 + P330 |
| RIDADR | NONH for all modes of transport |