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MK-571

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.

In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
ABCC1	MRP1	MK-571	3.5		2',7'-bis-(3-carboxy-propyl)-5-(and-6)-carboxyfluorescein (BCPCF)	human erythrocytes	Lania-Pietrzak, 2005
ABCC5	MRP5	MK-571	17		5-fluorodeoxyuridine monophosphate	MRP5-expressing HEK293 vesicles	Pratt, 2005
ABCC4	MRP4	MK-571	10		9-(2-phosphonomethoxyethyl)adenine (PMEA)	MRP4-expressing HEK293 vesicles	Reid, 2003
ABCC5	MRP5	MK-571	200		9-(2-phosphonomethoxyethyl)adenine (PMEA)	MRP4-expressing HEK293 vesicles	Reid, 2003
SLCO1B3	OATP1B3, OATP8	MK-571	0.5	0.2	Amanitin	MDCK II-OATP1B3	Letschert, 2006
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	MK-571	5		Bromsulphthalein	MDCK II-OATP1B1	Letschert, 2006
SLCO1B3	OATP1B3, OATP8	MK-571	0.3		Bromsulphthalein	MDCK II-OATP1B3	Letschert, 2006
SLCO2B1	OATP2B1, OATP-B	MK-571	0.2		Bromsulphthalein	MDCK II-OATP2B1	Letschert, 2006
ABCC1	MRP1	MK-571	5		Calcein AM	MDCK II-MRP1	Wortelboer, 2003
ABCC2	MRP2, cMOAT	MK-571	20.7		Calcein AM	MRP2-expressing MDCK-II cells	Leyers, 2008
ABCC5	MRP5	MK-571	15.9		Carboxydichlorofluorescein	MRP5-expressing HEK293 vesicles	Pratt, 2006
ABCC2	MRP2, cMOAT	MK-571	1		Chloromethylfluorescein-diacetate	MRP2-expressing MDCK cells	Kuhnle, 2009
ABCC4	MRP4	MK-571	~2		Cholyltaurine	MRP4-expressing V79 vesicles	Rius, 2003
ABCC1	MRP1	MK-571		134.7	Doxorubicin	2008/P-MRP1	Wong, 2009
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	MK-571	0.3		Estradiol-17beta-glucuronide	HEK293-OATP1B1	Yamazaki, 2005
ABCC2	MRP2, cMOAT	MK-571	10		Estradiol-17beta-glucuronide	MRP2-expressing sf9 vesicles	Pedersen, 2008
ABCC3	MRP3	MK-571	9.3		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	MK-571	6		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	MK-571	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	MK-571	4		Ethacrynic acid glutathione	MRP2-expressing Sf9 vesicles	Yamazaki, 2005
ABCC2	MRP2, cMOAT	MK-571	50		Irinotecan	Caco-2	Luo, 2002
ABCC1	MRP1	MK-571	0.6		Leukotriene C4	MRP1-expressing HeLa vesicles	Leier, 1994
ABCC2	MRP2, cMOAT	MK-571		13.1	Leukotriene C4	MRP2-expressing LLC-PK1 vesicles	Chen, 1999
ABCC2	MRP2, cMOAT	MK-571	4		Para-aminohippurate	MRP2-expressing HEK vesicles	Leier, 2000
ABCB11	BSEP	MK-571	3.53		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
ABCC2	MRP2, cMOAT	MK-571		26.4	Vinblastine	MDCK II-MRP2	Tang, 2002

Clinical Drug-Drug Interactions

No drug-drug interaction information.