Monocarboxylate transporters (MCT)
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MCT1 inhibitor
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.
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MCT1 and MCT2 inhibitor
AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.
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- Charlotte Petersen, .et al. MCT1 and MCT4 Expression and Lactate Flux Activity Increase During White and Brown Adipogenesis and Impact Adipocyte Metabolism, Sci Rep, 2017, 7: 13101 PMID: 29026134
- Kong SC, .et al. Monocarboxylate Transporters MCT1 and MCT4 Regulate Migration and Invasion of Pancreatic Ductal Adenocarcinoma Cells, Pancreas, 2016, Aug;45(7):1036-47 PMID: 26765963
- Anne Poder, .et al. Roles of acid-extruding ion transporters in regulation of breast cancer cell growth in a 3-dimensional microenvironment, Mol Cancer, 2016, 15: 45 PMID: 27266704
- Eumorphia G. Konstantakou, .et al. 3-BrPA eliminates human bladder cancer cells with highly oncogenic signatures via engagement of specific death programs and perturbation of multiple signaling and metabolic determinants, Mol Cancer, 2015, 14: 135 PMID: 26198749
- Álvarez Z, .et al. Neurogenesis and vascularization of the damaged brain using a lactate-releasing biomimetic scaffold., Biomaterials., 2014, 35(17):4769-81 PMID: 24636215
- Álvarez Z, .et al. Neuronal Progenitor Maintenance Requires Lactate Metabolism and PEPCK-M-Directed Cataplerosis., Cereb Cortex., 2014, 26(3):1046-58 PMID: 25452568
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MCT inhibitor
CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.
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MCT1 inhibitor
AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.
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- Lu Gao, .et al. Trophoblast-derived Lactic Acid Orchestrates Decidual Macrophage Differentiation via SRC/LDHA Signaling in Early Pregnancy, Int J Biol Sci, 2022, Jan 1;18(2):599-616 PMID: 35002512
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MCT1 inhibitor
AR-C117977 is a potent MCT1 inhibitor, which can reduce vimmune responses both in vitro and in vivo, maintains long-term graft survival, and induces operational tolerance.
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MCT inhibitor
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
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MCT Inhibitor
7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
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- Daniel Gundel, .et al. Preclinical Evaluation of [18F]FACH in Healthy Mice and Piglets: An 18F-Labeled Ligand for Imaging of Monocarboxylate Transporters with PET, Int J Mol Sci, 2021, Feb; 22(4): 1645 PMID: 33562048
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MCT Inhibitor
UK 5099 is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
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