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DC_517

Catalog No.GC32872

DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.

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DC_517 Chemical Structure

Cas No.: 500017-70-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$358.00
In stock
2mg
$214.00
In stock
5mg
$321.00
In stock
10mg
$552.00
In stock
50mg
$1,655.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of DC_517

DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.

DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively. DC_517 (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. DC_517 (0, 0.75, 1.5, and 3 μM) also dose-dependently induces apoptotic cell death in HCT116 cells[1].

[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):9028-9041.

Protocol of DC_517

Kinase experiment:

To measure the effects of DC_517 on mouse DNMT1 activity, 200 nM purified DNMT1 is incubated with 200 μM of DC_517 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):9028-9041.

Chemical Properties of DC_517

Cas No. 500017-70-9 SDF
Canonical SMILES OC(CNC(C)C)COC(CN1C(C=CC=C2)=C2C3=C1C=CC=C3)CN(C4=CC=CC=C45)C6=C5C=CC=C6
Formula C33H35N3O2 M.Wt 505.65
Solubility DMSO : ≥ 50 mg/mL (98.88 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of DC_517

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1 mg 5 mg 10 mg
1 mM 1.9777 mL 9.8883 mL 19.7765 mL
5 mM 0.3955 mL 1.9777 mL 3.9553 mL
10 mM 0.1978 mL 0.9888 mL 1.9777 mL
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In vivo Formulation Calculator (Clear solution) of DC_517

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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