ar-c155858

Description: AR-C155858 is a novel, selective and potent inhibitor of monocarboxylate transporters MCT1 and MCT2 with Kis of 2.3 nM and 10 nM, respectively. It binds to an intracellular site involving transmembrane helices 7-10. Inhibitor titrations of L-lactate transport by MCT1 in rat erythrocytes were used to determine the Ki and number of AR-C155858-binding sites (Et) on MCT1 and the turnover number of the transporter (kcat). Derived values were 2.3+/-1.4 nM, 1.29+/-0.09 nmol per ml of packed cells and 12.2+/-1.1 s-1 respectively.

References:

1. OvensMJ, et al. The inhibition of monocarboxylate transporter 2 (MCT2) byAR-C155858 is modulated by the associated ancillary protein. Biochem J.2010 Oct 15; 431(2):217-25.

2. OvensMJ, et al. AR-C155858 is a potent inhibitor of monocarboxylatetransporters MCT1 and MCT2 that binds to an intracellular site involvingtransmembrane helices 7-10. Biochem J. 2010 Jan 15; 425(3):523-30.

3. VijayN, et al. A Novel Monocarboxylate Transporter Inhibitor as a PotentialTreatment Strategy for gamma-Hydroxybutyric Acid Overdose. Pharm Res. 2015Jun; 32(6):1894-906.

4. Using the 'reverse Warburg effect' to identify high-risk breast cancer patients: stromal MCT4 predicts poor clinical outcome in triple-negative breast cancers. Cell Cycle. 2012 Mar 15; 11(6):1108-17.