Monocarboxylate Transporters

Monocarboxylate transporters (MCT) catalyze the bidirectional proton-linked transport of short-chain monocarboxylates such as L-lactate, ketone bodies and pyruvate across the plasma membrane of mammalian cells. MCT1-4 are key in the regulation of many cellular processes.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5658 AR-C 141990 hydrochloride
MCT1 inhibitor
4960 AR-C155858
MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells
5029 CHC
MCT inhibitor; decreases glycoloysis
5431 SR 13800
Potent MCT1 inhibitor
4186 UK 5099
MCT inhibitor; also inhibits of pyruvate transport

Related Targets

    There are 14 members of the solute carrier 16 (SLC16) gene family, four of which (SLC16A1, SLC16A3, SLC16A7 and SLC16A8) encode monocarboxylate transporters; MCT1, MCT4*, MCT2 and MCT3* respectively. MCTs have been shown to transport short-chain monocarboxylates such as L-lactate, ketone bodies and pyruvate across the plasma membrane of mammalian cells. MCTs have 12 transmembrane domains (TMDs) which consist of an intracellular N- and C-terminal and a large intracellular loop between TMDs 6 and 7. MCT1-4 require an ancillary protein either basigin or embigin, in order to express a fully functional protein at the plasma membrane.

    MCTs are fundamental in the regulation of many processes including pH, respiration, glycolysis and gluconeogenesis. MCT1 is expressed in most tissues and facilitates lactic acid uptake for oxidation in cardiac and red skeletal muscle. MCT2 is a high affinity transporter; its expression is more limited than MCT1 and varies between species. MCT3 expression is confined to the basal membrane of the retinal pigment epithelium and choroid plexus epithelia. MCT4 is a low affinity transporter and is mainly expressed in highly glycolytic cells, such as white muscle fibers. Many cells can up regulate MCT4 expression under hypoxic conditions; this is mediated through transcriptional control by HIF-1α.

    MCTs play a major role in the maintenance of the glycolytic metabolism through transport of lactate. MCT inhibitors have been shown to decrease glycolytic metabolism, migration and invasion, affect proliferation and induce cell death in certain cell lines. They are also useful tools for studying the Warburg effect.

    *Note: MCT3 has the synonym MCT4 and MCT4 has the synonym MCT5; for further details please view Genecards

    External sources of pharmacological information for Monocarboxylate Transporters :

      Literature for Monocarboxylate Transporters

      Cancer

      Cancer Research Product Guide

      A collection of over 750 products for cancer research, the guide includes research tools for the study of:

      • Cancer Metabolism
      • Epigenetics in Cancer
      • Receptor Signaling
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      • Invasion and Metastasis

      Monocarboxylate transporters Gene Data

      Gene Species Gene Symbol Gene Accession No. Protein Accession No.
      MCT1 Human SLC16A1 NM_003051 P53985
      Mouse Slc16A1 NM_009196 P53986
      Rat Slc16A1 NM_012716 NP_036848
      MCT2 Human SLC16A7 NM_004731 O60669
      Mouse Slc16A7 NM_011391 O70451
      Rat Slc16A7 NM_017302 NP_058998
      MCT3 (also know as MCT4) Human SLC16A8 NM_004207 O15427
      Mouse Slc16A8 NM_030696 P57787
      Rat Slc16A8 NM_030834 NP_110461
      MCT4 (also known as MCT5) Human SLC16A3 NM_004696 O15374
      Mouse Slc16A3 NM_146136 Q8R0M8
      Rat Slc16A3 NM_001013913 NP_001013935