| Description | Coumberone is a metabolic fluorogenic probe and isoform-selective substrate for all AKR1C isoforms. It can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone is a valuable tool for researching AKR1C. |
| In vitro | Coumberone (30 μM; 24 hours; HCT116 cells) is an AKR1C3 substrate and demonstrates maximal rates at ~10 μM[1].Coumberone (5 μM; 24 hours; COS-1 cells) can be used for the selective optical readout of each isoform, either AKR1C2 or AKR1C3[2].Coumberone (5 μM; 24 hours; IMR32 cells) enables real-time imaging of AKR1C induction[2].Coumberone (80 hours; IMR-32 cells) metabolism is indeed increased. Coumberone exhibits 10-fold greater catalytic efficiency for AKR1C3 than AKR1C2 in vitro[2]. Immunofluorescence[2]Cell Line: IMR32 cells Concentration: 5 μM Incubation Time: 24 hours Result: Enabled real-time imaging of AKR1C induction. |
| molecular weight | 345.398 |
| Molecular formula | C22H19NO3 |
| CAS | 878019-47-7 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Jamieson SM, et al. A novel fluorometric assay for aldo-keto reductase 1C3 predicts metabolic activation of the nitrogen mustard prodrug PR-104A in human leukaemia cells. Biochem Pharmacol. 2014;88(1):36-45. 2. Halim M, et al. Imaging induction of cytoprotective enzymes in intact human cells: coumberone, a metabolic reporter for human AKR1C enzymes reveals activation by panaxytriol, an active component of red ginseng. J Am Chem Soc. 2008;130(43):14123-14128. |