Ko143
E852343
Ko143 is a potent and selective small-molecule inhibitor of the breast cancer resistance protein (BCRP/ABCG2) efflux transporter used in research to study and overcome multidrug resistance.
Statements (46)
| Predicate | Object |
|---|---|
| instanceOf |
ABCG2 inhibitor
ⓘ
BCRP inhibitor ⓘ chemosensitizer ⓘ research chemical ⓘ small-molecule inhibitor ⓘ |
| affects | drug efflux mediated by BCRP ⓘ |
| associatedWith | multidrug resistance in oncology research ⓘ |
| discoveredAs | derivative of fungal toxin fumitremorgin C ⓘ |
| effect |
increases intracellular accumulation of BCRP substrates
ⓘ
reverses BCRP-mediated drug resistance ⓘ |
| fieldOfUse |
drug transport and disposition research
ⓘ
oncology research ⓘ pharmacology research ⓘ |
| hasAdvantage | reduced neurotoxicity compared with fumitremorgin C in preclinical studies ⓘ |
| hasProperty |
high potency against BCRP
ⓘ
high selectivity for BCRP over other ABC transporters ⓘ non-competitive BCRP inhibition (commonly reported) ⓘ |
| hasSynonym |
Ko 143
ⓘ
Ko-143 ⓘ |
| mechanismOfAction | inhibition of BCRP/ABCG2 efflux transporter activity ⓘ |
| roleInResearch |
positive control in BCRP inhibition assays
ⓘ
reference inhibitor in transporter selectivity panels ⓘ tool compound to validate BCRP involvement in drug transport ⓘ |
| selectivityProfile |
more selective for BCRP than for MRP1
ⓘ
more selective for BCRP than for P-glycoprotein ⓘ |
| speciesStudiedIn |
human-derived cell lines
ⓘ
mouse models ⓘ rat models ⓘ |
| targets |
ABCG2
NERFINISHED
ⓘ
BCRP NERFINISHED ⓘ breast cancer resistance protein NERFINISHED ⓘ |
| transportersComparedWith |
MRP1 (ABCC1)
NERFINISHED
ⓘ
P-glycoprotein (ABCB1) NERFINISHED ⓘ |
| usedFor |
in vitro transporter inhibition assays
ⓘ
in vivo transporter inhibition studies ⓘ overcoming multidrug resistance in cancer models ⓘ study of multidrug resistance mechanisms ⓘ |
| usedIn |
animal models of drug resistance
ⓘ
cancer cell line studies ⓘ transfected cell systems expressing ABCG2 ⓘ |
| usedTo |
assess drug–drug interaction risk via BCRP inhibition
ⓘ
characterize pharmacokinetics of BCRP substrates ⓘ |
| usedWith |
BCRP substrate chemotherapeutic agents
ⓘ
SN-38 ⓘ mitoxantrone NERFINISHED ⓘ topotecan NERFINISHED ⓘ |
Referenced by (1)
Full triples — surface form annotated when it differs from this entity's canonical label.