MCT4 Inhibitor

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.

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.

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).

MSC-4381 (MCT4-IN-1), a chemical probe, is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC₅₀ of 77 nM and a K_i 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.

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.

slCeMM1 is a selective SLC16A3 (MCT4) inhibitor. slCeMM1 inhibits lactate transport, induces intracellular lactate accumulation, reduces viability of SLC16A3-dependent cells, and inhibits growth of SLC16A3-dependent cells. slCeMM1 can be used for the research of rheumatoid arthritis and cancer.

PEG9MA10-PAB10-GalMA10 is a CD147 LYTAC degrader. PEG9MA10-PAB10-GalMA10 binds to the asialoglycoprotein receptor (ASGPR) via its galactose methacrylate domain, mediating its uptake by hepatoma cells. PEG9MA10-PAB10-GalMA10 induces lysosome-dependent degradation of CD147, resulting in concurrent loss of associated MCT1 and MCT4. PEG9MA10-PAB10-GalMA10 reduces extracellular lactate levels, increases intracellular lactate accumulation, inhibits glycolytic activity, and enhances mitochondrial respiratory capacity. PEG9MA10-PAB10-GalMA10 decreases the secretion of MMP-2 and MMP-9, and upregulates the expression of E-cadherin. PEG9MA10-PAB10-GalMA10 exhibits anti-tumor efficacy in hepatoma models. PEG9MA10-PAB10-GalMA10 can be used for research on liver cancer (hepatocellular carcinoma).

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.