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Catalog No. Product Name Information Product Use Citations Product Validations
S7339 AZD3965 AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.
Biomark Res, 2024, 12(1):48
Cell Rep, 2024, 43(9):114686
J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363
S8612 α-cyano-4-hydroxycinnamic acid(α-CHCA) 4-Chloro-α-cyanocinnamic acid (α-CHCA) is a classic monocarboxylate transporters (MCT) inhibitor. α-cyano-4-hydroxycinnamate (CHC) has a 10-fold selectivity for MCT1 compared to other MCTs.
J Exp Clin Cancer Res, 2024, 43(1):105
Cancer Cell Int, 2024, 24(1):5
Int J Mol Sci, 2023, 24(1)737
S8747 BAY-8002 BAY-8002 is a novel MCT1 inhibitor and potently suppress bidirectional lactate transport. BAY-8002 significantly increases intratumor lactate levels and transiently modulates pyruvate levels.
Cell Chem Biol, 2023, 30(8):953-964.e9
Nat Commun, 2022, 13(1):5184
Cancers (Basel), 2021, 13(14)3635
S9907 Syrosingopine Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.
S9929 VB124 VB124, a potent and selective MCT4 inhibitor, specifically inhibits lactate efflux/import in MDA-MB-231 cells expressing MCT4, and is used for the research of cardiac hypertrophy, heart failure, and metabolism. 
Cardiovasc Diabetol, 2024, 23(1):96
J Orthop Surg Res, 2023, 18(1):131
E1549 AZD0095 AZD0095 is a selective and orally active Monocarboxylate transporter 4 (MCT4) inhibitor with IC50 of 1.3 nM and effectively inhibits the tumor growth in NCI-H358 xenografts in combination with Cediranib.
E1751New MSC-4381 MSC-4381 (MCT4-IN-1) is an orally active, selective inhibitor of monocarboxylate transporter 4 (MCT4) with an IC50 of 77 nM and a Ki of 11 nM. It has the potential to inhibit lactate efflux and promote intracellular lactate accumulation in MCT4-expressing cell lines.
S7919 AR-C155858 AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Ki value of 2.3 nM and 10 nM, respectively.
bioRxiv, 2024, 10.1101/2024.01.25.577208
S6732 7ACC2 7ACC2 is a potent inhibitor of mitochondrial pyruvate transport 1 (MCT1) with an IC50 value of 10 nM for lactate uptake in SiHa human cervix carcinoma cells.
S7339 AZD3965 AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.
Biomark Res, 2024, 12(1):48
Cell Rep, 2024, 43(9):114686
J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363
S8612 α-cyano-4-hydroxycinnamic acid(α-CHCA) 4-Chloro-α-cyanocinnamic acid (α-CHCA) is a classic monocarboxylate transporters (MCT) inhibitor. α-cyano-4-hydroxycinnamate (CHC) has a 10-fold selectivity for MCT1 compared to other MCTs.
J Exp Clin Cancer Res, 2024, 43(1):105
Cancer Cell Int, 2024, 24(1):5
Int J Mol Sci, 2023, 24(1)737
S8747 BAY-8002 BAY-8002 is a novel MCT1 inhibitor and potently suppress bidirectional lactate transport. BAY-8002 significantly increases intratumor lactate levels and transiently modulates pyruvate levels.
Cell Chem Biol, 2023, 30(8):953-964.e9
Nat Commun, 2022, 13(1):5184
Cancers (Basel), 2021, 13(14)3635
S9907 Syrosingopine Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.
S9929 VB124 VB124, a potent and selective MCT4 inhibitor, specifically inhibits lactate efflux/import in MDA-MB-231 cells expressing MCT4, and is used for the research of cardiac hypertrophy, heart failure, and metabolism. 
Cardiovasc Diabetol, 2024, 23(1):96
J Orthop Surg Res, 2023, 18(1):131
E1549 AZD0095 AZD0095 is a selective and orally active Monocarboxylate transporter 4 (MCT4) inhibitor with IC50 of 1.3 nM and effectively inhibits the tumor growth in NCI-H358 xenografts in combination with Cediranib.
E1751New MSC-4381 MSC-4381 (MCT4-IN-1) is an orally active, selective inhibitor of monocarboxylate transporter 4 (MCT4) with an IC50 of 77 nM and a Ki of 11 nM. It has the potential to inhibit lactate efflux and promote intracellular lactate accumulation in MCT4-expressing cell lines.
S7919 AR-C155858 AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Ki value of 2.3 nM and 10 nM, respectively.
bioRxiv, 2024, 10.1101/2024.01.25.577208
S6732 7ACC2 7ACC2 is a potent inhibitor of mitochondrial pyruvate transport 1 (MCT1) with an IC50 value of 10 nM for lactate uptake in SiHa human cervix carcinoma cells.
E1751New MSC-4381 MSC-4381 (MCT4-IN-1) is an orally active, selective inhibitor of monocarboxylate transporter 4 (MCT4) with an IC50 of 77 nM and a Ki of 11 nM. It has the potential to inhibit lactate efflux and promote intracellular lactate accumulation in MCT4-expressing cell lines.

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