Catalog Number: 4960
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.
Technical Data
  • M.Wt:
    461.53
  • Formula:
    C21H27N5O5S
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    496791-37-8
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca UK Limited
Background References
  1. 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
  2. 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
  3. Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis.
    Doherty et al.
    Cancer Res., 2014;74:908
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AR-C155858 include:

1 Citations: Showing 1 - 1

  1. 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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