mct4

VB124 is an orally active, potent and selective MCT4 inhibitor. VB124 blocked lactate import (IC50 value of 8.6 nM) and export (IC50 value of 19 nM) in MDA-MB-231 cells. VB124 is selective for MCT4 over MCT1 and shows minimal MCT1 inhibitory activity in MCT1-expressing BT20 cells (IC50 value of 24 μM).

AZD0095 is a selective inhibitor of MCT4 with an IC50 of 1.3 nM.

MSC-4381 (MCT4-IN-1) is an orally available and selectively modeled highly potent inhibitor of monocarboxylic acid transporter protein 4 (MCT4 SLC16A3) with potential anticancer and antitumor activity for the study of osteosarcoma.

MCT-IN-1 (compound 2) acts as a potent inhibitor of the monocarboxylate transporter (MCT), demonstrating IC50 values of 9 nM for MCT1 and 14 nM for MCT4.

Syrosingopine is a dual inhibitor of MCT1 and MCT4, 60 times more potent against MCT4, preventing lactate and H+ efflux. Syrosingopine is an orally available antihypertensive drug with potential for cancer research in combination with metformin.