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.
Sold for research purposes under agreement from AstraZeneca UK Limited
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
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
2 Citations for AR-C155858
Citations are publications that use Tocris products. Selected citations for AR-C155858 include:
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
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
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Reviews for AR-C155858
Average Rating: 3 (Based on 1 Review.)
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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
Literature in this Area
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