Monocarboxylate Transporter 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.

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.

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 K_i 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.

H-HomoArg-OH (L-Homoarginine) is an orally active endogenous non-protein amino acid. H-HomoArg-OH acts as a weak alternative substrate for NOS and interferes with NO production, selectively inhibits tissue-nonspecific alkaline phosphatase (TNAP), and suppresses the uptake of arginine by y⁺-type transporters (system y⁺). H-HomoArg-OH increases tissue hArg concentrations in vivo, regulates amino acid homeostasis, and improves renal function and pathological features of diabetic nephropathy. H-HomoArg-OH can be used in studies related to diabetes and cardiomyopathy.

N-Acetyl-R-leucine is an amino-protecting group N-substituted chiral amino acid. N-Acetyl-R-leucine is a PepT1 and MCT1 inhibitor with IC₅₀ of 0.74 and 11 mM, respectively. N-Acetyl-R-leucine can be used for LysoTracker signaling studies.

H-HomoArg-OH-¹³C₇,¹⁵N₄ hydrochloride (L-Homoarginine-¹³C₇,¹⁵N₄ hydrochloride) is the ¹⁵N, ¹³C-labeled H-HomoArg-OH (hydrochloride) (HY-W012340). H-HomoArg-OH hydrochloride (L-Homoarginine hydrochloride) is an orally active endogenous non-protein amino acid. H-HomoArg-OH hydrochloride acts as a weak alternative substrate for NOS and interferes with NO production, selectively inhibits tissue-nonspecific alkaline phosphatase (TNAP), and suppresses the uptake of arginine by y⁺-type transporters (system y⁺). H-HomoArg-OH hydrochloride increases tissue hArg concentrations in vivo, regulates amino acid homeostasis, and improves renal function and pathological features of diabetic nephropathy. H-HomoArg-OH hydrochloride can be used in studies related to diabetes and cardiomyopathy.

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).

Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2.

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.

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.

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.

Acriflavine (Acriflavinium chloride) hydrochloride is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic agent. Acriflavine hydrochloride is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine hydrochloride inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine hydrochloride is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2.

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

H-HomoArg-OH hydrochloride (L-Homoarginine hydrochloride) is an orally active endogenous non-protein amino acid. H-HomoArg-OH hydrochloride acts as a weak alternative substrate for NOS and interferes with NO production, selectively inhibits tissue-nonspecific alkaline phosphatase (TNAP), and suppresses the uptake of arginine by y⁺-type transporters (system y⁺). H-HomoArg-OH hydrochloride increases tissue hArg concentrations in vivo, regulates amino acid homeostasis, and improves renal function and pathological features of diabetic nephropathy. H-HomoArg-OH hydrochloride can be used in studies related to diabetes and cardiomyopathy.

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.

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.