KO143

KO143 is a highly potent, selective, and specific small-molecule inhibitor of the Breast Cancer Resistance Protein (BCRP), also known as ATP-binding cassette sub-family G member 2 (ABCG2). Structurally, it is a tetracyclic analog of the fungal toxin fumitremorgin C. KO143 is primarily utilized as a research 'tool inhibitor' to investigate the role of ABCG2 in multidrug resistance (MDR), drug pharmacokinetics, and the integrity of the blood-brain and blood-cerebrospinal fluid barriers. By binding to the central cavity of the ABCG2 transporter, KO143 prevents the ATP-dependent efflux of a wide range of xenobiotics, chemotherapeutic agents (such as mitoxantrone and topotecan), and endogenous substrates. Despite its high potency in vitro and in animal models, its potential for clinical application is limited by rapid metabolic degradation, specifically the carboxylesterase 1-mediated hydrolysis of its t-butyl ester moiety.

Other names

fumitremorgin C analogABCG2 inhibitorABCG-2 inhibitorABCG 2 inhibitorBCRP inhibitor