Synonyms:
(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino-[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
BMLEI3960005
BMLEI3960025
ENZOBMLEI3960005
ENZOBMLEI3960025
Ko143 ≥96% (par HPLC)
Ko143
Analog of the fungal toxin fumitremorgin C. Potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP, EC90=26nM). Highly effective for increasing the intracellular drug accumulation and reversing BCRP-mediated multidrug resistance yet has little activity against P-glycoprotein, multidrug resistance-associated protein (MRP1) and other known drug transporters. In mouse models Ko143 was able to restore the intracellular accumulation and abolish the directionality in net flux of dasatinib. It is a highly useful tool for the identification of drug transport processes in complex experimental systems.
White solid.
Soluble in DMSO (>25mg/ml) or 100% ethanol (>25mg/ml).