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
Biological ActivityAR-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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
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.
Citations for AR-C155858
The citations listed below are publications that use Tocris products. Selected citations for AR-C155858 include:
5 Citations: Showing 1 - 5
Lactate and pyruvate promote oxidative stress resistance through hormetic ROS signaling.
Authors: Tauffenberger Et al.
Cell Death Dis 2019;10:653
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
Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake.
Authors: Diaz-Garcia Et al.
Cell Metab 2017;26:361
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
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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