Description: BAY-8002 is a potent dual MCT1/2 inhibitor (IC50 values are 3, 8, and 12 nM at rat (C6), human (DLD-1) and mouse (4T1) MCT1 respectively). Target: Monocarboxylate transporter. Smiles: OC(=O)c1ccccc1NC(=O)c1cc(ccc1Cl)S(=O)(=O)c1ccccc1. References: Quanz M, et al. Preclinical Efficacy of the Novel...

BAY-8002 is an inhibitor of monocarboxylate transporter 1 (MCT1, IC50 = 11.4 nM). It inhibits lactate uptake in DLD-1 cells expressing human MCT1 (IC50 = 85 nM) but not Evsa-T cells expressing human MCT4 (IC50 = >50 µM). It inhibits the proliferation of 24 cancer cell lines when used at a concentration of 10 µM....