Dibenzylfluorescein

Dibenzylfluorescein is a fluorogenic probe with the excitation wavelength of 485nm and emission wavelength of 535nm ^[1]. Dibenzylfluorescein acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19), and is typically used near the apparent Km value of 0.87-1.9µM^{[1, 2]}. Dibenzylfluorescein is suitable for use in the progress curve analysis approach and can be used as an initial screen to identify compounds that require more detailed investigations in drug interaction optimization^[3]. Dibenzylfluorescein can be used to develop cell-based assays to simultaneously assess enzyme activity, protein half-life, cell viability, and screen inhibitors with slow dissociation rates^[4].

References:
[1] Work H M, Kandel S E, Lampe J N. Characterization of fluorescent probe substrates to develop an efficient high-throughput assay for neonatal hepatic CYP3A7 inhibition screening[J]. Scientific Reports, 2021, 11(1): 19443.
[2] Stresser D M, Blanchard A P, Turner S D, et al. Substrate-dependent modulation of CYP3A4 catalytic activity: analysis of 27 test compounds with four fluorometric substrates[J]. Drug Metabolism and Disposition, 2000, 28(12): 1440-1448.
[3] Salminen K A, Leppänen J, Venäläinen J I, et al. Simple, direct, and informative method for the assessment of CYP2C19 enzyme inactivation kinetics[J]. Drug metabolism and disposition, 2011, 39(3): 412-418.
[4] Heidary D K, Kriger S M, Hachey A C, et al. A fluorometric CYP19A1 (aromatase) activity assay in live cells[J]. ChemMedChem, 2021, 16(18): 2845-2850.

Dibenzylfluorescein是一种荧光探针，激发波长为485nm，发射波长为535nm^[1]。Dibenzylfluorescein作为特定细胞色素P450（CYP）亚型的底物，包括CYP3A4、CYP2C8、CYP2C9、CYP2C19和芳香化酶（CYP19），通常在接近表观K_m值0.87-1.9µM的范围内使用^{[1, 2]}。Dibenzylfluorescein适用于进度曲线分析方法，可作为初步筛选工具，以识别需要在药物相互作用优化中进行更详细研究的化合物^[3]。Dibenzylfluorescein可用于开发基于细胞的检测方法，以同时评估酶活性、蛋白半衰期、细胞活力，并筛选具有慢解离速率的抑制剂^[4]。