1. Metabolic Enzyme/Protease
  2. PDHK

Dicoumarol (Synonyms: Dicumarol)

Cat. No.: HY-N0645 Purity: 98.70%
Handling Instructions

Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.

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

Dicoumarol Chemical Structure

Dicoumarol Chemical Structure

CAS No. : 66-76-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.

IC50 & Target

IC50: 0.37 μM (NQO1)[1], 19.42 μM (PDK1)[2]

In Vitro

Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37±0.15 and 19.42±0.032 μM, respectively. The PDK1 activity is inhibited by Dicoumarol in a dose-dependent manner. The enzymatic activity of PDK1 is reduced by approximately 94% when treated with 200 μM Dicoumarol. Dicoumarol decreases the p-PDHA1 level by 26% (100 μM Dicoumarol) and by 72% (200 μM Dicoumarol), with no statistical difference in the total PDHA1 level. Both 100 μM and 200 μM Dicoumarol markedly induce apoptosis of SKOV3 cells. Similarly, flow cytometric analysis of annexin V+PI+ cells reveals that 100 μM and 200 μM Dicoumarol treatments generate approximately 20.87% and 24.94% apoptotic cells, respectively, significantly higher than vehicle treatment[2]. It is also observed that treatment of MCF-7-TAMR cells with Dicoumarol, a known NQO1 inhibitor, reverses their tamoxifen-resistance phenotype[3].

In Vivo

Dichloroacetate (DCA) at 100 mg/kg, Dicoumarol at 30 mg/kg, and Dicoumarol at 50 mg/kg all significantly reduce tumor volume and decrease tumor weight, when compare to tumors from control or vehicle groups. Total caspase-3 and total anti-poly (ADP-ribose) polymerase (PARP) are significantly decreased in Dicoumarol-treated SKOV3 xenografts, when compare to tumors from the control or vehicle group[2].

Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (19.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9736 mL 14.8681 mL 29.7362 mL
5 mM 0.5947 mL 2.9736 mL 5.9472 mL
10 mM 0.2974 mL 1.4868 mL 2.9736 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

The in vitro cell viability is examined using the standard MTT assay. SKOV3 or A2780 cells are seeded in 96-well plates at 8000 cells/well. The next day, increasing concentrations of Dicoumarol (DIC) are added into each well, and the plate is incubated for 24 h. Then, 10 μL of 10 mg/mL MTT reagent in phosphate-buffered saline (PBS) is added into each well, and the plate is incubated for an additional 4 h. The formazan crystals are dissolved in 150 μL of DMSO, and after the plate is shaken for 5 min, the optical density at 570 nm is recorded by the reader[2].

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

Animal Administration
[2]

Twenty five female BALB/c-nu mice aged 5 to 6 weeks old and weighing approximately 15 g each are used. A total of 1×107 SKOV3 cells are subcutaneously injected into the upper flank. After 10 days, when the tumor volume reaches approximately 100 mm3, the nude mice are randomized into five groups (n=5/group) and are given the following treatments intraperitoneally (i.p.) every other day, for a total of 12 days: control group, administered with 0.2 mL of 0.9% NaCl; vehicle group, administered with 1 mM NaOH; dichloroacetate (DCA) group, administered with 100 mg/kg DCA; Dicoumarol (DIC)-30 group, administered with 30 mg/kg Dicoumarol; and Dicoumarol-50 group, administered with 50 mg/kg Dicoumarol. The body weights and tumor volumes of each mouse are monitored every other day until sacrifice (on day 12 after the initial treatment)[2].

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

References
Molecular Weight

336.29

Formula

C₁₉H₁₂O₆

CAS No.

66-76-2

SMILES

O=C1C(CC2=C(O)C3=CC=CC=C3OC2=O)=C(O)C4=CC=CC=C4O1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Dicoumarol
Cat. No.:
HY-N0645
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Dicoumarol

Cat. No.: HY-N0645