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High level of intracellular glutathione (GSH) has been identified as a major barrier for cancer therapy. Therefore, effective regulation of GSH can be regarded as a novel approach for cancer therapy. In this study, an off-on fluorescent probe (NBD-P) is developed for selective and sensitive sensing GSH. NBD-P has a good cell membrane permeability that can be applied in bioimaging endogenous GSH in living cells. Moreover, the NBD-P probe is used to visualize GSH in animal models. In addition, a rapid drug screening method is successfully established using the fluorescent probe NBD-P. A potent natural inhibitor of GSH is identified as Celastrol from Tripterygium wilfordii Hook F, which effectively triggers mitochondrial apoptosis in clear cell renal cell carcinoma (ccRCC). More importantly, NBD-P can selectively respond to GSH fluctuations to distinguish cancer tissues from normal tissues. Thus, the present study provides insights into fluorescence probes for the screening GSH inhibitors and cancer diagnosis, as well as in-depth exploration of the anti-cancer effects of Traditional Chinese Medicine (TCM). [Display omitted] • NBD-P has a good cell membrane permeability that can be applied in GSH bioimaging in living cells. • NBD-P exhibits distinguished imaging capability in vivo and can specific monitor GSH fluctuations in clinical diagnosis. • A visual screening method was established by NBD-P , and Celastrol is identified as a natural inhibitor of GSH. • Celastrol triggers apoptosis in clear cell renal cell carcinoma by reducing GSH level and ROS generation. [ABSTRACT FROM AUTHOR]