2. Epigenetics
  3. DNA Methyltransferase
  4. 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.

For research use only. We do not sell to patients.

DC_517 Chemical Structure

DC_517 Chemical Structure

CAS No. : 500017-70-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 467 In-stock
Solution
10 mM * 1 mL in DMSO USD 467 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 720 In-stock
50 mg USD 2160 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

DC_517 Related Antibodies

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DNA Methyltransferase DNMT1 DNMT3 MGMT

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1]

DNMT1

0.91 μM (Kd)

DNMT1

1.7 μM (IC50)

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DC_517 Related Antibodies
Molecular Weight

505.65

Formula

C33H35N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(CNC(C)C)COC(CN1C(C=CC=C2)=C2C3=C1C=CC=C3)CN(C4=CC=CC=C45)C6=C5C=CC=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (98.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.25 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 3.25 mg/mL (6.43 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9777 mL 9.8883 mL 19.7765 mL 49.4413 mL
5 mM 0.3955 mL 1.9777 mL 3.9553 mL 9.8883 mL
10 mM 0.1978 mL 0.9888 mL 1.9777 mL 4.9441 mL
15 mM 0.1318 mL 0.6592 mL 1.3184 mL 3.2961 mL
20 mM 0.0989 mL 0.4944 mL 0.9888 mL 2.4721 mL
25 mM 0.0791 mL 0.3955 mL 0.7911 mL 1.9777 mL
30 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6480 mL
40 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.2360 mL
50 mM 0.0396 mL 0.1978 mL 0.3955 mL 0.9888 mL
60 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL
80 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6180 mL
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DC_517 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DC_517500017-70-9DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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