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 (5):

Cat. No. Product Name Effect Purity
  • HY-12750
    AZD3965 Inhibitor
    AZD3965 is a selective MCT1 inhibitor, it inhibits MCT1 with a binding affinity (Ki) 1.6 nM and it is 6 fold selective over MCT2 and does not inhibit MCT3 or 4 at 10 μM concentrations.
  • HY-13248
    AR-C155858 Inhibitor
    AR-C155858 is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.
  • HY-15475
    UK-5099 Inhibitor
    UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
  • 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-D0713
    7ACC2 Inhibitor
    7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.