2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. Monocarboxylate Transporter
  5. MCT4 Isoform

MCT4

Monocarboxylate transporter 4 (MCT4) also known as solute carrier family 16 member 3 (SLC16A3). MCT4 acts as an H+/lactate exporter in highly glycolytic tissues. In fact, MCT4 was first identified as a key component of lactate efflux in highly glycolytic white fiber myocytes, and was later demonstrated to show a high affinity for lactate over other monocarboxylates, as referenced by its comparatively lower Km for lactate. Furthermore, MCT4 has been shown to be overexpressed in diverse types of neoplasia, among malignant gliomas. Mechanistically, MCT4 is upregulated under hypoxia via binding of HIF-1α to two hypoxic response elements (HRE) within the SLC16A3 promoter. This process enables tumor cells, including those within the core of the heterogeneous tumor mass to survive, despite being at a distance from blood vessels that supply their metabolic needs.

MCT4 Related Products (4):

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.
  • 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.
  • 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).
  • 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. 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.