AR-C155858
Chemical Name: 6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Purity: ≥98%
Biological Activity
AR-C155858 is an inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and <10 nM respectively). Exhibits no activity at MCT4. Blocks proliferation of Raji lymphoma cells in vitro. Inhibits glycolysis and glutathione synthesis in cancer cells.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis.
Doherty et al.
Cancer Res., 2014;74:908 -
The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein.
Ovens et al.
Biochem.J., 2010;431:217 -
AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.
Ovens et al.
Biochem.J., 2010;425:523
Product Datasheets
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Citations for AR-C155858
The citations listed below are publications that use Tocris products. Selected citations for AR-C155858 include:
18 Citations: Showing 1 - 10
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Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix.
Authors: Sandra L Et al.
iScience 2023;26:105965
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High glucose promotes regulatory T cell differentiation.
Authors: Adam J Et al.
PLoS One 2023;18:e0280916
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Lactate Rewires Lipid Metabolism and Sustains a Metabolic-Epigenetic Axis in Prostate Cancer.
Authors: Matteo Et al.
Cancer Res 2022;82:1267-1282
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Autoregulation of H+/lactate efflux prevents monocarboxylate transport (MCT) inhibitors from reducing glycolytic lactic acid production.
Authors: Wiktoria Et al.
Br J Cancer 2022;127:1365-1377
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Protein lactylation induced by neural excitation.
Authors: Atsushi Et al.
Cell Rep 2021;37:109820
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MCT1 Deletion in Oligodendrocyte Lineage Cells Causes Late-Onset Hypomyelination and Axonal Degeneration.
Authors: Jeffrey D Et al.
Cell Rep 2021;34:108610
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CAIX forms a transport metabolon with monocarboxylate transporters in human breast cancer cells.
Authors: Holger M Et al.
Oncogene 2020;39:1710-1723
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Impairment of Glycolysis-Derived l-Serine Production in Astrocytes Contributes to Cognitive Deficits in Alzheimer's Disease.
Authors: Charles Et al.
Cell Metab 2020;31:503-517.e8
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Defective Mitochondrial Pyruvate Flux Affects Cell Bioenergetics in Alzheimer's Disease-Related Models.
Authors: Emy Et al.
Cell Rep 2020;30:2332-2348.e10
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A glycolytic shift in Schwann cells supports injured axons.
Authors: Keit Men Et al.
Nat Neurosci 2020;23:1215-1228
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Cancer-associated fibroblasts promote prostate cancer malignancy via metabolic rewiring and mitochondrial transfer.
Authors: Maria Letizia Et al.
Oncogene 2019;38:5339-5355
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Lactate and pyruvate promote oxidative stress resistance through hormetic ROS signaling.
Authors: Tauffenberger Et al.
Cell Death Dis 2019;10:653
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Glucose and lactate as metabolic constraints on presynaptic transmission at an excitatory synapse.
Authors: Bruce P Et al.
J Physiol 2018;596:1699-1721
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The Glia-Neuron Lactate Shuttle and Elevated ROS Promote Lipid Synthesis in Neurons and Lipid Droplet Accumulation in Glia via APOE/D.
Authors: Liu Et al.
Cell Metab 2017;26:719
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Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake.
Authors: Diaz-Garcia Et al.
Cell Metab 2017;26:361
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Type 2 Diabetes Variants Disrupt Function of SLC16A11 through Two Distinct Mechanisms.
Authors: Steven A Et al.
Cell 2017;170:199-212.e20
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Hypoxia-induced carbonic anhydrase IX facilitates lactate flux in human breast cancer cells by non-catalytic function.
Authors: Jamali Et al.
Sci Rep 2015;5:13605
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Lactate Regulates Metabolic and Pro-inflammatory Circuits in Control of T Cell Migration and Effector Functions.
Authors: Haas Et al.
Nat Commun 2015;13:e1002202
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To transiently block uptake capacity of MCT receptors in small intestine of in an ex vivo rodent model
Only partial blockage achieved at selected concentration
