MCT1 Inhibitor

AZD3965 is a selective MCT1 inhibitor with a K_i of 1.6 nM, showing 6-fold selectivity over MCT2.

AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with K_is of 2.3 nM and 10 nM, respectively.

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.

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.

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.

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).

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.

MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity.

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.