Coumberone 是一种代谢荧光探针，对所有 AKR1C 亚型具有异构体选择性。AKR1C 家族的所有四个成员都能将 couberone 还原为其荧光醇 couberol。Coumberone 可用于 AKR1C 的研究。
货号:ajcx33452
CAS:878019-47-7
分子式:C22H19NO3
分子量：345.39
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C[1][2].

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].

[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.