. 2020 Apr;72(2):466–485. doi: 10.1124/pr.119.018762

TABLE 3.

Substrates and inhibitors of monocarboxylate transporters

Km, Ki, and IC₅₀ values were obtained from the listed references and Morris and Felmlee (2008).

Isoform	Species	Expression System	Substrate	Km (mM)	Inhibitor	Ki or IC₅₀ (µM)	References
MCT1	Human	Caco-2	Hesperetin	NA			Shen et al., 2015
		Xenopus oocytes	Lactate	3.5–6	Phloretin	28^a	Bröer et al., 1998; Lin et al., 1998; Juel and Halestrap, 1999; Cuff et al., 2002; Cundy et al., 2004; Nancolas et al., 2016; Curtis et al., 2017
			Pyruvate	1.8–2.5	Quercetin	NA
			α-Ketoisovalerate	1.3	CHC	425^a
			α-Oxoisohexanoate	0.67	pCMBS	NA
			α-Oxoisovalerate	1.25	XP13512	0.62^b
			Butyrate	9	Lonidamine	36.8^a
			XP13512	0.22
		Jurkat membranes			AZD3965	0.0016^a
	Rat	MDA-MB231	GHB	4.6	Phloretin	28^b	Bröer et al., 1998, 1999; Wang et al., 2006a
		Xenopus oocytes	Lactate	3.5	Quercetin	14^b
			GHB	4.6	Benzobromaron	22^b
					CHC	425^b
MCT2	Human	Xenopus oocytes	Pyruvate	0.025	CHC	NA	Lin et al., 1998; Nancolas et al., 2016
					L-Lactate	NA
					GHB	NA
					Lonidamine	36.4^a
	Rat	Xenopus oocytes	Lactate	0.74	Phloretin	14^b	Broer et al., 1999; Curtis et al., 2017
			Pyruvate	NA	Quercetin	5^b
					Benzobromaron	9^b
					CHC	24^b
		Recombinant MCT2-expressing yeast membranes			AZD3965	0.020^a
MCT3	Human	ARPE-19 cells	Lactate	NA			Philp et al., 2003
MCT4	Human	Xenopus oocytes	L-lactate	28	pCMBS	21^a	Manning Fox et al., 2000; Kobayashi et al., 2006; Nancolas et al., 2016
			D-lactate	519	CHC	991^a
			Pyruvate	153	Phloretin	41^a
			D-β-hydroxybutyrate	130	NPPB	240^a
			Acetoacetate	216	Fluvastatin	32^b
			α-Ketobutyrate	57	Atorvastatin	32^b
			α-Ketoisocaproate	95	Lovastatin	44^b
			α-Ketoisovalerate	113	Simvastatin	79^b
					Lonidamine	40.4^a
	Rat	Xenopus oocytes	L-lactate	34	CHC	350^b	Dimmer et al., 2000
			Pyruvate	36	pCMBS	NA
			2-Oxoisohexanoate	13
			Acetoacetate	31
			β-Hydroxybutyrate	65
MCT5			Unknown
MCT6	Human	Xenopus oocytes	Bumetanide	0.084	Furosemide	46^b	Murakami et al., 2005; Kohyama et al., 2013
			Nateglinide	0.046	Azosemide	21^b
			Prostaglandin F₂α	NA	Piretanide	163^b
			Probenecid	NA	Torasemide	13^b
					Thiazides	NA
					Probenecid	NA
					Glibenclamide	NA
					Nateglinide	5.4^a
					Quercetin	25^b	Jones et al., 2017
					Luteolin	NA
					Phloretin	23^a, 17^b
					Morin	33^b
MCT7	Human		Ketone bodies (β-hydroxybutyrate)	NA			Hugo et al., 2012
MCT7	Zebrafish		Ketone bodies (β-hydroxybutyrate)	NA			Hugo et al., 2012
MCT8	Human	COS1 and JEG3 cells	T₃	NA			Friesema et al., 2006
	Human	COS1 and JEG3 cells	T₄	NA			Friesema et al., 2006
	Rat	Xenopus oocytes	T₃	NA	N-bromoacetyl-T₃	NA	Friesema et al., 2003
	Rat	Xenopus oocytes	T₄	NA	Bromosulfophthalein	NA	Friesema et al., 2003
MCT9			Carnitine	NA			Jones and Morris, 2016
MCT10	Rat	Xenopus oocytes	L-Trytophan	3.8			Kim et al., 2001
			L-Tyrosine	2.6
			L-Phenylalanine	7.0
			L-DOPA	6.4
MCT11			Unknown				Jones and Morris, 2016
MCT12	Human	Xenopus oocytes	Creatinine	0.57			Abplanalp et al., 2013
	Rat		Creatinine	NA			Abplanalp et al., 2013
MCT13			Unknown				Jones and Morris, 2016
MCT14			Unknown				Jones and Morris, 2016

CHC, α-cyano-4-hydroxycinnamate; GHB, gamma-hydroxybutyric acid; NA, not available; NPPB, 5-nitro-2-(3-phenylpropylamino)benzoic acid; pCMBS, p-chloromercuribenzene sulfonate.

^{^a}

Ki.

^{^b}

IC₅₀.