| 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 |
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| 2018-0101 |
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| 2018-0101 |
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| 2018-0101 |
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