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.

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.