| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
DNMT1 (DNA methyltransferase 1). IC50 = 10.3 μM; Kd = 1.09 μM.
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|---|---|
| ln Vitro |
The inhibitor DC-05 inhibits DNA methyltransferase 1 (DNMT1) and has an IC50 of 10.3 μM and a Kd of 1.09 μM, respectively. DNMT3A, DNMT3B, G9a, SUV39H1, MLL1, SET7/9, and PRMT1 are all targets of DC-05's poor activity (IC50: >200, >200, >150, >150, >150, 37.1 μM). After 24, 48, and 72 hours of treatment, DC-05 (1.25, 2.5, 5 and 10 μM) efficiently suppresses the growth of human pancreatic cancer Capan-1 and human colon cancer HCT116 [1].
DC_05 inhibits DNMT1 with an IC50 of 10.3 μM and a Kd of 1.09 μM. It is selective for DNMT1 over other DNA methyltransferases and protein methyltransferases. By inhibiting DNMT1, it reduces DNA methylation, which can reactivate silenced genes and inhibit cancer cell proliferation. |
| ln Vivo |
In vivo, DC_05 has been studied for its anti-cancer activity. It effectively inhibits the proliferation of cancer cells and has potential as a therapeutic agent for cancers involving aberrant DNA methylation. However, specific in vivo data are limited.
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| Enzyme Assay |
DC_05 is evaluated in cell-free assays using purified DNMT1 enzyme. The compound is incubated with DNMT1, a DNA substrate, and the methyl donor S-adenosylmethionine (SAM). The inhibition of DNA methylation is measured using radioactive or fluorescence-based methods. IC50 and Kd values are determined.
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| Cell Assay |
DC_05 is assessed in cell-based assays using cancer cell lines such as HCT116 and Capan-1. Cells are treated with DC_05 (1.25, 2.5, 5, and 10 μM) for 24, 48, and 72 hours. Cell proliferation is measured using MTT or other assays. DNA methylation levels and gene expression changes are also assessed.
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| Animal Protocol |
DC_05 is administered in animal models of cancer to evaluate its anti-tumor efficacy. Efficacy is assessed by measuring tumor growth inhibition and changes in DNA methylation in tumor tissues. Pharmacokinetic studies are conducted to assess bioavailability and tissue distribution.
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| ADME/Pharmacokinetics |
No detailed PK data available. DC_05 has a molecular weight of 383.49.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. For research use only.
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| References | |
| Additional Infomation |
DC_05 is a selective DNMT1 inhibitor. Molecular formula: C22H21N3O4; MW: 383.49. For research use only.
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| Molecular Formula |
C25H25N3O
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|---|---|
| Molecular Weight |
383.49
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| Exact Mass |
383.199
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| CAS # |
890643-16-0
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| Related CAS # |
890643-16-0
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| PubChem CID |
16451230
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
667.5±55.0 °C at 760 mmHg
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| Flash Point |
357.5±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
5.41
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
506
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LJWMTSMUQJNHOC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H25N3O/c29-19(16-26-14-13-18-15-27-23-10-4-1-7-20(18)23)17-28-24-11-5-2-8-21(24)22-9-3-6-12-25(22)28/h1-12,15,19,26-27,29H,13-14,16-17H2
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| Chemical Name |
1-((2-(1H-Indol-3-yl)ethyl)amino)-3-(9H-carbazol-9-yl)-propan-2-ol
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| Synonyms |
DC-05 DC_05 DC05 DC 05
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~260.76 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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