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Monocarboxylate Transporters

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Monocarboxylate transporters (MCTs) constitute a family of proton-linked plasma membrane transporters that carry molecules having one carboxylate group (monocarboxylates), such aslactate and pyruvate, across biological membranes. Highly malignant tumors rely heavily on aerobic glycolysis (metabolism of glucose to lactic acid even under ample tissue oxygen; Warburg Effect) and thus need to efflux lactic acid via MCTs to the tumor micro-environment to maintain a robust glycolytic flux and to prevent the tumor from being "pickled to death". The MCTs have been successfully targeted in pre-clinical studies using RNAi and a small-molecule inhibitor alpha-cyano-4-hydroxycinnamic acid (ACCA; CHC) to show that inhibiting lactic acid efflux is a very effective therapeutic strategy against highly glycolytic malignant tumors.

Products Related to Monocarboxylate Transporters(14)

  • GC10680 structure
    GC10680AR-C155858
    CAS: 496791-37-8
    Purity: >98.00%

    AR-C155858 is a potent inhibitor of monocarboxylate transporter 1 (MCT1) with a K i value of 2.3nM, and also inhibits MCT2 with a K i value of >10nM.

  • GC10877 structure
    GC10877α-Cyano-4-hydroxycinnamic acid (CHC)
    CAS: 28166-41-8
    Purity: >98.00%

    CHC (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs).

  • GC11010 structure
    GC11010AZD 3965
    CAS: 1448671-31-5
    Purity: >98.00%

    AZD 3965 is a potent, orally active, and selective inhibitor of monocarboxylate transporter 1 (MCT1), with a K i value of 1.6nM.

  • GC13691 structure
    GC136917ACC1
    CAS: 50995-74-9
    Purity: >99.50%

    MCT inhibitor

  • GC14642 structure
    GC146427ACC2
    CAS: 1472624-85-3
    Purity: >98.00%

    MCT inhibitor

  • GC19488 structure
    GC19488BAY-8002
    CAS: 724440-27-1
    Purity: >98%

    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC 50 of 85nM.

  • GC39536 structure
    GC39536Syrosingopine
    CAS: 84-36-6
    Purity: >99.00%

    Syrosingopine is a dual MCT1 and MCT4 inhibitor, with IC 50 values of 2.5μM and 0.04μM, respectively.

  • GC50163 structure
    GC50163SR 13800
    CAS: 227321-12-2
    Purity: >99.00%

    SR 13800 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. SR 13800 has anti-cancer activity.

  • GC50226 structure
    GC50226AR-C 141990 hydrochloride
    CAS: 2250019-94-2
    Purity: >98.00%

    MCT1 inhibitor

  • GC63062 structure
    GC63062MCT4-IN-1
    CAS: 2445185-57-7
    Purity: >98.00%

    MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research.

  • GC63496 structure
    GC63496VB124
    CAS: 2230186-18-0
    Purity: >99.00%

    VB124 is a safe, effective and orally active selective monocarboxylate transport protein 4(MCT4) inhibitor. VB124 blocks the input (IC 50 = 8.6nM) and output (IC 50 = 19nm) of lactic acid in MDA-MB-231 cells.

  • GC68713 structure
    GC68713AZD0095
    CAS: 2750001-23-9
    Purity: >99.50%

    AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). When used in combination with Cediranib, AZD0095 effectively inhibits tumor growth of NCI-H358 xenografts.

  • GC73305 structure
    GC73305MCT-IN-1
    CAS: 1685273-57-7
    Purity: >98.00%

    MCT-IN-1 (compound 2) is a potent inhibitor of monocarboxylate transporter (MCT), with the IC50 of 9 nM and 14 nM for MCT1 and MCT4, respectively.

  • GC79495 structure
    GC79495slCeMM1
    CAS: 949973-22-2
    Purity: >98%

    slCeMM1 is a selective SLC16A3 ( MCT4 ) inhibitor.