| S7339 |
AZD3965
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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.
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Cell Host Microbe, 2025, 33(7):1089-1105.e7
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Nat Commun, 2025, 16(1):6999
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Cell Commun Signal, 2025, 23(1):364
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| S8612 |
α-cyano-4-hydroxycinnamic acid(α-CHCA)
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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.
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Nucleic Acids Res, 2025, 53(17)gkaf882
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BMC Med, 2025, 23(1):331
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Cell Commun Signal, 2025, 23(1):364
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| S8747 |
BAY-8002
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BAY-8002 is a novel MCT1 inhibitor and potently suppress bidirectional lactate transport. This compound significantly increases intratumor lactate levels and transiently modulates pyruvate levels.
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Genes Dis, 2025, 12(4):101554
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Cell Metab, 2024, S1550-4131(24)00415-7
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Cell Chem Biol, 2023, 30(8):953-964.e9
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| S9907 |
Syrosingopine
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Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.
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Genes Dis, 2025, 12(4):101554
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Cancer Metab, 2025, 13(1):9
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| S9929 |
VB124
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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.
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Cancer Metab, 2025, 13(1):9
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Cardiovasc Diabetol, 2024, 23(1):96
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J Orthop Surg Res, 2023, 18(1):131
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| E1549 |
AZD0095
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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.
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| E8301New |
MCT-IN-1
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MCT-IN-1 (compound 2) is a potent and selective inhibitor of monocarboxylate transporter (MCT), with the IC50 of 9 nM and 14 nM for MCT1 and MCT4, respectively. It can be used in research as a potential target for overcoming multidrug resistance (MDR) in cancer.
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| E1751 |
MSC-4381
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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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| S7919 |
AR-C155858
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AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Ki value of 2.3 nM and 10 nM, respectively.
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J Cereb Blood Flow Metab, 2025, 0271678X251328179
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bioRxiv, 2024, 10.1101/2024.01.25.577208
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| S6732 |
7ACC2
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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.
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