mct

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

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).

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.

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.

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.

Tempoacmcta is a peptide.

Maresin conjugates in tissue regeneration 1 (MCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is then converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase. MCTR1 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR1 (50 ng/mouse, i.p.) prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR1 reduces the amount of eicosanoids in the exudate.

Maresin conjugates in tissue regeneration 2 (MCTR2) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase then to MCTR2 by γ-glutamyl transferase. MCTR2 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR2 prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR2 selectively reduced the amount of the eicosanoids PGD2 and PGF2α in the exudate.

Maresin conjugates in tissue regeneration 3 (MCTR3) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase, then to MCTR2 by γ-glutamyl transferase, and to MCTR3 by dipeptidase. MCTR3 accelerates tissue regeneration in planaria (1 and 100 nM) approximately as potently as MCTR2 and more potently than MCTR1. Pretreatment with MCTR3 prior to E. coli administration in mice reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR3 selectively reduces the amount of the eicosanoids PGD2 , PGE2 , PGF2α , and TXB2 in the exudate.

IMCTA-C14, a detergent and derivative of the microbial metabolite 4-trehalosamine, exhibits a critical micelle concentration (CMC) of 0.11 mM and a hydrophilic-lipophilic balance (HLB) value of 9.72. It effectively extracts proteins, including membrane proteins, from OVK18 ovarian cancer cells at concentrations of 0.05 and 0.5%. Furthermore, IMCTA-C14 demonstrates antibacterial activity against various bacterial strains (MICs = 8-128 µg/ml) and shows cytotoxicity against a spectrum of 52 cancer cell lines (IC50s = 2.9-29.2 µg/ml). At a concentration of 50 µM, it induces autophagy in OVK18 cells.

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

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

m-C-tri(CH2-PEG1-NHS ester) is a non-cleavable one-unit polyethylene glycol (PEG) linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

PSMA617-TCMC is a derivative of PSMA-617 with structure modification, in which the caroboxy groups in DOTA ring is replaced by TCMC macrocycle. PSMA-617 is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer.

Boc-LRR-AMC TFA is a fluorescent protease substrate used to detect the trypsin-like activity of the 26S proteasome or 20S proteasome core.

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).

H-β-Ala-AMC TFA is a substrate for aminopeptidase and serves as a building block for synthesizing the fluorogenic vanin I substrate [pantothenate-AMC].

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

N-CBZ-Phe-Arg-AMC TFA (Z-FR-AMC TFA) is a fluorescent substrate for serine proteases, which releases free AMC upon protease cleavage. Its excitation/emission wavelengths are 380/460 nm, and it can be used to assess the activity of trypsin, plasmin, and cathepsin.

Pyr-Arg-Thr-Lys-Arg-AMC TFA, an AMC-tagged decapeptide, is selectively cleaved by proteases such as trypsin and thrombin, serving as a substrate for measuring protease activity and assessing enzyme inhibitor efficacy [1].

Z-Gly-Gly-Arg-AMC TFA (66216-78-2 free base) is a thrombin-specific fluorogenic substrate used to assess thrombin generation in platelet-rich plasma (PRP) and platelet-poor plasma (PPP).

MC-Thailanstatin A serves as a drug-linker conjugate for ADC (Antibody-Drug Conjugates) synthesis. It is utilized in the formation of ADCs [1].

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