Cat. No. 4960

AR-C155858 C21H27N5O5S [496791-37-8]

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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 Activity

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

Soluble to 100 mM in DMSO
>98 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Doherty et al (2014) Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis. Cancer Res. 74 908. PMID: 24285728.

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.

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Citations are publications that use Tocris products. Selected citations for AR-C155858 include:

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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Keywords: AR-C155858, supplier, monocarboxylate, transporters, MCT1, MCT2, inhibitors, inhibits, Tocris Bioscience, Monocarboxylate Transporter Inhibitor products

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