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Dicoumarol (Dicoumarin) is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively. 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.
In vivo, Dicoumarol at 30 mg/kg and 50 mg/kg all significantly reduce tumor volume and decrease tumor weight, when compare to tumors from control or vehicle groups.
| Molecular Weight | 336.29 |
| Formula | C19H12O6 |
| CAS Number | 66-76-2 |
| Solubility (25°C) | DMSO 3.3 mg/mL Ethanol: 12 mg/mL Water 15 mg/mL (ultrasonic and adjust pH to 11 with NaOH) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDK1 Products |
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| OSU-03012
OSU-03012 is a novel and potent, blood-brain permeable inhibitor of PDK-1 with an IC50 of 5 µM. |
| GSK2334470
GSK2334470 is a highly specific and potent inhibitor of PDK1 with IC50 of 10 nM. |
| BX-795
BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitor with IC50 of 6 nM, 41 nM and 111 nM, respectively. |
| BX-912
BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM. |
| AZD7545
AZD7545 is a potent PDHK inhibitor with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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