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Submit ReviewAR-C155858
Description: MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells
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% (HPLC)
Biological Activity for AR-C155858
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.
Licensing Information
Sold for research purposes under agreement from AstraZeneca UK Limited
Technical Data for AR-C155858
| M. Wt | 461.53 |
| Formula | C21H27N5O5S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 496791-37-8 |
| PubChem ID | 10226546 |
| InChI Key | ISIVOJWVBJIOFM-ZDUSSCGKSA-N |
| Smiles | O=C(N4OC[C@@H](O)C4)C1=C(CC3=C(C)NN=C3C)SC(N2CC(C)C)=C1C(N(C)C2=O)=O |
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.
Solubility Data for AR-C155858
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.15 | 100 |
Preparing Stock Solutions for AR-C155858
The following data is based on the product molecular weight 461.53. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.17 mL | 10.83 mL | 21.67 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets for AR-C155858
References for AR-C155858
References are publications that support the biological activity of the product.
Ovens et al (2010) The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem.J. 431 217 PMID: 20695846
Ovens et al (2010) AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem.J. 425 523 PMID: 19929853
Doherty et al (2014) Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis. Cancer Res. 74 908 PMID: 24285728
If you know of a relevant reference for AR-C155858, please let us know.
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Keywords: AR-C155858, AR-C155858 supplier, monocarboxylate, transporters, MCT1, MCT2, inhibitors, inhibits, Monocarboxylate, Transporters, 4960, Tocris Bioscience
18 Citations for AR-C155858
Citations are publications that use Tocris products. Selected citations for AR-C155858 include:
Adam J et al (2023) High glucose promotes regulatory T cell differentiation. PLoS One 18 e0280916 PMID: 36730267
Sandra L et al (2023) Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix. iScience 26 105965 PMID: 36824274
Diaz-Garcia et al (2017) Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake. Cell Metab 26 361 PMID: 28768175
Liu et al (2017) The Glia-Neuron Lactate Shuttle and Elevated ROS Promote Lipid Synthesis in Neurons and Lipid Droplet Accumulation in Glia via APOE/D. Cell Metab 26 719 PMID: 28965825
Haas et al (2015) Lactate Regulates Metabolic and Pro-inflammatory Circuits in Control of T Cell Migration and Effector Functions. Nat Commun 13 e1002202 PMID: 26181372
Jamali et al (2015) Hypoxia-induced carbonic anhydrase IX facilitates lactate flux in human breast cancer cells by non-catalytic function. Sci Rep 5 13605 PMID: 26337752
Jeffrey D et al (2021) MCT1 Deletion in Oligodendrocyte Lineage Cells Causes Late-Onset Hypomyelination and Axonal Degeneration. Cell Rep 34 108610 PMID: 33440165
Atsushi et al (2021) Protein lactylation induced by neural excitation. Cell Rep 37 109820 PMID: 34644564
Tauffenberger et al (2019) Lactate and pyruvate promote oxidative stress resistance through hormetic ROS signaling. Cell Death Dis 10 653 PMID: 31506428
Bruce P et al (2018) Glucose and lactate as metabolic constraints on presynaptic transmission at an excitatory synapse. J Physiol 596 1699-1721 PMID: 29430661
Steven A et al (2017) Type 2 Diabetes Variants Disrupt Function of SLC16A11 through Two Distinct Mechanisms. Cell 170 199-212.e20 PMID: 28666119
Wiktoria et al (2022) Autoregulation of H+/lactate efflux prevents monocarboxylate transport (MCT) inhibitors from reducing glycolytic lactic acid production. Br J Cancer 127 1365-1377 PMID: 35840734
Matteo et al (2022) Lactate Rewires Lipid Metabolism and Sustains a Metabolic-Epigenetic Axis in Prostate Cancer. Cancer Res 82 1267-1282 PMID: 35135811
Maria Letizia et al (2019) Cancer-associated fibroblasts promote prostate cancer malignancy via metabolic rewiring and mitochondrial transfer. Oncogene 38 5339-5355 PMID: 30936458
Holger M et al (2020) CAIX forms a transport metabolon with monocarboxylate transporters in human breast cancer cells. Oncogene 39 1710-1723 PMID: 31723238
Emy et al (2020) Defective Mitochondrial Pyruvate Flux Affects Cell Bioenergetics in Alzheimer's Disease-Related Models. Cell Rep 30 2332-2348.e10 PMID: 32075767
Charles et al (2020) Impairment of Glycolysis-Derived l-Serine Production in Astrocytes Contributes to Cognitive Deficits in Alzheimer's Disease. Cell Metab 31 503-517.e8 PMID: 32130882
Keit Men et al (2020) A glycolytic shift in Schwann cells supports injured axons. Nat Neurosci 23 1215-1228 PMID: 32807950
Do you know of a great paper that uses AR-C155858 from Tocris? Please let us know.
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Oocyte inhibition.
By
Murali K Yanda on 11/13/2023
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Oocytes
Inhibition of L-lactate transport activity at pH 6 by increasing concentrations of AR-C155858 was determined using 0.5 mM L-[14C]lactate (pH 6).
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