TABLE 3

Substrates and inhibitors of monocarboxylate transporters

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

IsoformSpeciesExpression SystemSubstrateKm (mM)InhibitorKi or IC50 (µM)References
MCT1HumanCaco-2HesperetinNAShen et al., 2015
Xenopus oocytesLactate3.5–6Phloretin28aBröer 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
Pyruvate1.8–2.5QuercetinNA
α-Ketoisovalerate1.3CHC425a
α-Oxoisohexanoate0.67pCMBSNA
α-Oxoisovalerate1.25XP135120.62b
Butyrate9Lonidamine36.8a
XP135120.22
Jurkat membranesAZD39650.0016a
RatMDA-MB231GHB4.6Phloretin28bBröer et al., 1998, 1999; Wang et al., 2006a
Xenopus oocytesLactate3.5Quercetin14b
GHB4.6Benzobromaron22b
CHC425b
MCT2HumanXenopus oocytesPyruvate0.025CHCNALin et al., 1998; Nancolas et al., 2016
L-LactateNA
GHBNA
Lonidamine36.4a
RatXenopus oocytesLactate0.74Phloretin14bBroer et al., 1999; Curtis et al., 2017
PyruvateNAQuercetin5b
Benzobromaron9b
CHC24b
Recombinant MCT2-expressing yeast membranesAZD39650.020a
MCT3HumanARPE-19 cellsLactateNAPhilp et al., 2003
MCT4HumanXenopus oocytesL-lactate28pCMBS21aManning Fox et al., 2000; Kobayashi et al., 2006; Nancolas et al., 2016
D-lactate519CHC991a
Pyruvate153Phloretin41a
D-β-hydroxybutyrate130NPPB240a
Acetoacetate216Fluvastatin32b
α-Ketobutyrate57Atorvastatin32b
α-Ketoisocaproate95Lovastatin44b
α-Ketoisovalerate113Simvastatin79b
Lonidamine40.4a
RatXenopus oocytesL-lactate34CHC350bDimmer et al., 2000
Pyruvate36pCMBSNA
2-Oxoisohexanoate13
Acetoacetate31
β-Hydroxybutyrate65
MCT5Unknown
MCT6HumanXenopus oocytesBumetanide0.084Furosemide46bMurakami et al., 2005; Kohyama et al., 2013
Nateglinide0.046Azosemide21b
Prostaglandin F2αNAPiretanide163b
ProbenecidNATorasemide13b
ThiazidesNA
ProbenecidNA
GlibenclamideNA
Nateglinide5.4a
Quercetin25bJones et al., 2017
LuteolinNA
Phloretin23a, 17b
Morin33b
MCT7HumanKetone bodies (β-hydroxybutyrate)NAHugo et al., 2012
ZebrafishNA
MCT8HumanCOS1 and JEG3 cellsT3NAFriesema et al., 2006
T4NA
RatXenopus oocytesT3NAN-bromoacetyl-T3NAFriesema et al., 2003
T4NABromosulfophthaleinNA
MCT9CarnitineNAJones and Morris, 2016
MCT10RatXenopus oocytesL-Trytophan3.8Kim et al., 2001
L-Tyrosine2.6
L-Phenylalanine7.0
L-DOPA6.4
MCT11UnknownJones and Morris, 2016
MCT12HumanXenopus oocytesCreatinine0.57Abplanalp et al., 2013
RatCreatinineNAAbplanalp et al., 2013
MCT13UnknownJones and Morris, 2016
MCT14UnknownJones 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.