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.

SR13800 is a monocarboxylate transporter 1 (MCT1) inhibitor with cell-permeable.

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].

Syrosingopine has selective depleting effect on brain amines is potentiated by combined treatment with disulfiram or fusaric acid, a dopamine beta-hydroxylase inhibitor.

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

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).

Monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) were found to be potent inhibitors of mitochondrial respiration supported by pyruvate

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).

AR-C117977 is a potent MCT1 inhibitor, which can reduce vimmune responses both in vitro and in vivo, maintains long-term graft survival, and induces operational tolerance.

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