Monocarboxylate transporter

VB124 is an orally active, potent, and selective MCT4 inhibitor, demonstrating specificity in hindering lactate efflux, with IC50 values of 8.6 nM and 19 nM for lactate import and export, respectively, in MDA-MB-231 cells. Its high selectivity for MCT4 over MCT1 positions VB124 as a promising agent for researching cardiac hypertrophy, heart failure, and metabolic disorders [1].

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor. The solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) represents a promising target for the treatment of cancer. MCT1-IN-3 (compound 24) showed the highest MCT1 transport inhibition with an IC50 value of 81.0 Nm. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1.

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

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

D-Phenylalanine, a necessary aromatic amino acid, is a precursor of thyroxine, dopamine, melanin, and noradrenaline (norepinephrine).

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

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].

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.

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

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

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.

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).