1. Epigenetics
  2. DNA Methyltransferase
  3. DC_517

DC_517 

Cat. No.: HY-12747 Purity: 99.66%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 467 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2160 In-stock
Estimated Time of Arrival: December 31
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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].

Molecular Weight

505.65

Formula

C₃₃H₃₅N₃O₂

CAS No.

500017-70-9

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (98.88 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.1978 mL 0.9888 mL 1.9777 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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
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Keywords:

DC_517DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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DC_517
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HY-12747
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