monocarboxylate transporter

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

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).

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].

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

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.

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.

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

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

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).

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

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.

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

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.

KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells.