|Related Categories||Approved Therapeutics/Drug Candidates, Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience, Drug Efflux Pumps,|
|color||white to off-white|
|solubility||DMSO: >10 mg/mL|
|storage temp.||room temp|
Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone. The ABCG2 transporter breast cancer resistance protein (BCRP) plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. It increases intracellular drug accumulation and reverse BCRP-mediated multidrug resistance. It blocked topotecan and ABZSO transport in a concentration-dependent manner. Ko143 is reported to be a more specific inhibitor of BCRP than other known inhibitors of BCRP such as fumitremorgin C and GF120918.
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner.
Protein-based drug transporters are found in most tissues including liver, kidney, intestine, and brain. Because of their complexity and genetic heterogeneity, these proteins are often produced as re...
Biofiles Volume 6 Article 1
Keywords: Absorption, Anti-inflammatory agents, Antibiotics, Antimicrobials, Apoptosis, Cancer, Cytotoxins, Detoxification, Enzyme-linked immunosorbent assay, Gene expression, Genetic, High performance liquid chromatography, Immunohistochemistry, Mass spectrometry, Metabolites, Phosphorylations, Separation, Transfection, Western blot
ABCG2/BCRP decreases the transfer of a food-born chemical carcinogen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in perfused term human placenta. Myllynen P., et al. Toxicol. Appl. Pharmacol. 232, 210-217, (2008)
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