monocarboxylate transporter

AZD3965 (AZD-3965) belongs to small molecule inhibitors, serving as a monocarboxylate transporter 1 (MCT1) inhibitor (Ki=1.6 nM), with 6-fold higher selectivity for MCT1 over MCT2, featuring favorable selectivity, cell permeability, and oral activity, for antitumor research.

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.

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

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

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).

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.

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).

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.

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].

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.

Acriflavine Hydrochloride (Acriflavine HCl) is a HIF-1α inhibitor. It acts by targeting HIF-1α-mediated pathways and decreasing the level of PGK1, VEGF, and HIF-1α in vitro and in vivo.

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.

AR-C141990 is a lactate transporters inhibitor.

Silychristin (Silicristin) is a plant growth regulator. Silychristin is an anti-hepatotoxic agent. Silychristin is the inhibitor of horseradish peroxidases and lipoxygenase.

AR-C141990 hydrochloride is a potent inhibitor of lactate transporters known as monocarboxylate transporters (MCTs), with pK i values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. This compound also exhibits immunosuppressive properties and effectively inhibits the graft versus host response.

N-Acetyl-R-leucine is a useful organic compound for research related to life sciences. The catalog number is T66941 and the CAS number is 19764-30-8.

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.

AZ1422 is a selective MCT4 inhibitor, applicable for cancer research.

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.

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.

CPK peptide is a tumor-targeting peptide that specifically binds to the monocarboxylate transporter 1 (MCT1) receptor. The MCT1 receptor is overexpressed in many human colon cancer cell lines, while it is not present in normal cells. CPK peptide can be utilized in research related to tumor diagnostics.