tcsc0540 AR-C155858

AR-C155858 is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (K_i values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.

IC50 & Target: Ki: 2.3 nM (MCT1), 10 nM (MCT2)

In Vitro: AR-C155858 (10 nM-100 nM) inhibits MCT1/MCT2 C-terminal chimaeras^[1]. AR-C155858 inhibits MCT2, and the 70% inhibition seen at 10 nM is followed by a gradually increasing inhibition which can only be explained by a K_i value of significantly less than 10 nM. AR-C155858 inhibits MCT1 expressed in Xenopus oocytes in a time- and concentration-dependent manner^[2].