2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. Monocarboxylate Transporter
  5. MCT1 Isoform

MCT1

MCT1 (SLC16A1) is a proton-linked monocarboxylate transporter that mediates the bidirectional transmembrane movement of lactate, pyruvate, and ketone bodies, thereby supporting cellular metabolism and pH homeostasis[1][2]. Mechanistically, MCT1 participates in lactate shuttling between metabolically distinct cell populations and contributes to the maintenance of glycolytic flux through coordinated transport of monocarboxylates and protons[1][2]. Because lactate transport is a central component of metabolic adaptation, MCT1 has been extensively investigated in cancer models in which lactate exchange supports tumor growth and metabolic plasticity[3][4]. Inhibition of MCT1 disrupts lactate transport, alters glycolytic metabolite profiles, and suppresses tumor growth in multiple preclinical models[3][4]. Compared with related isoforms, MCT1 displays distinct substrate and inhibitor affinities, whereas MCT4 is relatively resistant to several widely used MCT1-directed inhibitors, creating important functional differences in lactate-handling networks[2][5]. This isoform selectivity is particularly relevant for experimental design because cellular responses to MCT1 blockade can depend on the presence or absence of compensatory MCT4 expression[4][5]. For experimental applications, AZD3965 is a first-in-class MCT1 inhibitor that induces intracellular lactate accumulation and has advanced into clinical evaluation, while AR-C155858 potently inhibits MCT1 and MCT2 through binding determinants located within transmembrane helices 7-10 but shows little activity against MCT4[4][5].

MCT1 Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-12750
    AZD3965
    		Inhibitor 99.96%
    AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.
  • HY-13248
    AR-C155858
    		Inhibitor 99.62%
    AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.
  • HY-N4115
    Syrosingopine
    		Inhibitor 99.52%
    Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine.
  • HY-D0067
    7ACC1
    		Inhibitor 99.94%
    7ACC1 (DEAC; Coumarin D 1421; D 1421) is a monocarboxylate transporter 1 (MCT-1)/MCT-4 specifc blocker. 7ACC1 attenuates renal cancer cell proliferation, migration, invasion and down-regulates the levels of MCT1/MCT4 expression and extracellular lactate. 7ACC1 is promising for research of cancers.
  • HY-122312
    BAY-8002
    		Inhibitor 98.84%
    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
  • HY-150314
    MCT-IN-1
    		Inhibitor 99.74%
    MCT-IN-1 (Compound 2) is a potent MCT inhibitor, with IC50 values of 9 nM and 14 nM against MCT1 and MCT4, respectively. MCT-IN-1 can be used in research related to solid tumors.
  • HY-18974
    MCT1-IN-2
    		Inhibitor 99.88%
    MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity.
  • HY-75625
    2-Hydroxy-4-methoxybenzoic acid
    		Inhibitor 99.64%
    2-Hydroxy-4-methoxybenzoic acid is an orally active inhibitor of MCT-1 and MCT-4, as well as a plant biomarker. 2-Hydroxy-4-methoxybenzoic acid can be isolated from roots. 2-Hydroxy-4-methoxybenzoic acid induces Apoptosis and loss of mitochondrial membrane potential. 2-Hydroxy-4-methoxybenzoic acid exhibits anticancer activity against breast cancer. 2-Hydroxy-4-methoxybenzoic acid normalizes lactic acid levels. 2-Hydroxy-4-methoxybenzoic acid neutralizes viper venom and attenuates its lethal, hemorrhagic, coagulant and anticoagulant activities in male albino mice. 2-Hydroxy-4-methoxybenzoic acid possesses antihyperlipidemic, antidiabetic and hepatoprotective activities.