Monocarboxylate transporter

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).

AZD3965 (AZD-3965) is a selective inhibitor of monocarboxylate transporter 1 (MCT1).

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

7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for [14C]-lactate influx; new antitumor treatment targeting lactate transport in Y cells.

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor, targeting solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) for cancer treatment. MCT1-IN-3 (compound 24) showed the highest MCT1 transport inhibition with an IC50 value of 81.0 Nm and also exhibits significant inhibitory activity against the multidrug transporter ABCB1.

AR-C155858 is an inhibitor of monocarboxylate transporter MCT1 and MCT2 (Kis: 2.3 nM and 10 nM).

α-Cyano-4-hydroxycinnamic acid (α-CHCA) is an inhibitor of monocarboxylate transporter 1 (MCT1), which blocks pyruvate transport in rat heart mitochondria (IC50: 1.5 μM).

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).

Coumarin343 inhibits monocarboxylic acid transporter protein 4 with IC50 values in the range of 0.01-100 µM.Coumarin343 exhibits anticancer and antibacterial activity.Coumarin343 is a coumarin dye.

Niflumic acid (Nifluril) is a Ca2+-activated Cl- channel blocker and an analgesic and anti-inflammatory agent used in the therapy of rheumatoid arthritis.

7ACC1 (D 142) selectively affects a single part of the MCT symporter translocation cycle, leading to strict inhibition of lactate influx. This singular activity is associated with antitumor effects less prone to resistance and side effects.

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.

Lactate Transporter 1 (Compound 1) serves as an active lactate transporter within living cells and exerts cytotoxic effects, exhibiting IC50 values of 3.36 μM in HeLa, 3.27 μM in CAL27, 5.58 μM in MCF7, and 7.66 μM in MCF10A cells. Additionally, an additive effect with Cisplatin has been observed in HeLa cells [1].