1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter

Monocarboxylate Transporter

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.

Monocarboxylate Transporter Related Products (16):

Cat. No. Product Name Effect Purity
  • HY-139665
    VB124 Inhibitor 99.86%
    VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism[1].
  • HY-N4115
    Syrosingopine Inhibitor 99.30%
    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[1][2].
  • HY-12750
    AZD3965 Inhibitor 99.95%
    AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.
  • HY-148517
    AZD0095 Inhibitor 99.59%
    AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1].
  • 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-D0067
    7ACC1 Inhibitor
    7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  • HY-122312
    BAY-8002 Inhibitor 98.39%
    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[1].
  • HY-155382
    Lactate transportor 1
    Lactate transportor 1 (compound 1) is an active lactate transporter in living cells. Lactate transportor 1 displays the cytotoxic effect, with IC50 values of 3.36, 3.27,5.58 and 7.66 μM in Hela, CAL27, MCF7 and MCF10A, respectively. Lactate transportor 1 has an additive effect with Cisplatin (HY-17394) observed in HeLa cells[1].
  • HY-160107
    AZ1422 Inhibitor
    AZ1422 is a selective MCT4 inhibitor that can be used in cancer research[1].
  • HY-D0713
    7ACC2 Inhibitor 99.62%
    7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux[1][2].
  • HY-132301
    MSC-4381 Inhibitor 98.89%
    MSC-4381 (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. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research[1]. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-148574
    MCT1-IN-3 Inhibitor
    MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer[1].
  • HY-N0647
    Silychristin 99.91%
    Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM[1][2].
  • HY-18974
    MCT1-IN-2 Inhibitor
    MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity[1][2].
  • HY-119996A
    AR-C141990 hydrochloride Inhibitor
    AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively[1]. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response[2].
  • HY-107641
    α-Cyano-4-hydroxycinnamic acid Inhibitor
    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications[1][2].