Monocarboxylate transporters (MCT)

AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.

UK 5099 is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.

AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.

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.

7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.

7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.

BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.

VB124 is a potent and selective inhibitor of monocarboxylate transporter 4 (MCT4), demonstrating significant activity with IC50 values of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 exhibits high selectivity for MCT4, distinguishing it from MCT1. This compound is valuable for research in areas such as cardiac hypertrophy, heart failure, and metabolic studies.

Syrosingopine is a dual inhibitor of lactate transporters MCT1 and MCT4, effectively reducing glycolytic metabolism in cancer cells when combined with metformin. This compound has been shown to induce synthetic lethality, making it a valuable tool for cancer research. Additionally, Syrosingopine exhibits anti-hypertensive properties by depleting peripheral norepinephrine stores, presenting further avenues for cardiovascular studies.

AZD0095 is a selective, orally bioavailable inhibitor of monocarboxylate transporter 4 (MCT4), characterized by an IC50 of 1.3 nM. This compound demonstrates significant antitumor activity by effectively inhibiting tumor growth in NCI-H358 xenograft models, particularly in combination with Cediranib. AZD0095 serves as a valuable tool for research into metabolic modulation and therapeutic strategies in cancer biology.

MSC-4381 is a selective inhibitor of monocarboxylate transporter 4 (MCT4/SLC16A3), exhibiting an IC50 of 77 nM and a Ki of 11 nM. This compound effectively inhibits lactate efflux and decreases cellular viability in cells with high MCT4 expression. MSC-4381 serves as a valuable tool for research involving MCT4 transporter inhibition and features a reactive alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

MCT-IN-1 is a potent inhibitor of monocarboxylate transporters (MCT1 and MCT4), exhibiting IC50 values of 9 nM and 14 nM, respectively. This compound is particularly relevant for research into solid tumors, offering valuable insights into metabolic modulation and therapeutic strategies targeting tumor microenvironments. MCT-IN-1 serves as a crucial tool for investigating the role of lactate transport in cancer cell proliferation and survival.

N-Acetyl-R-leucine is an N-substituted chiral amino acid that functions as an inhibitor of the peptides transporter PepT1 and the monocarboxylate transporter MCT1, with IC50 values of 0.74 mM and 11 mM, respectively. This compound is valuable for investigating transporter activity and can be utilized in LysoTracker signaling studies, contributing to research on cellular metabolism and related pathways.

MCT1-IN-2 is a potent inhibitor of monocarboxylate transporter 1 (MCT1), which plays a key role in cellular metabolism by facilitating the transport of lactate and other monocarboxylates. This compound has demonstrated significant anti-cancer activity, making it a valuable tool for research in cancer metabolism and therapeutic development. MCT1-IN-2 is suitable for studies investigating the role of MCT1 in tumor growth and progression, as well as potential combination therapies targeting metabolic pathways in cancer cells.

MCT1-IN-3 is a potent inhibitor of the monocarboxylate transporter 1 (MCT1), exhibiting an IC50 value of 81.0 nM. Additionally, this compound shows significant inhibitory activity against the multidrug transporter ABCB1. MCT1-IN-3 is valuable for research applications focused on cancer, particularly in elucidating the role of MCT1 in tumor metabolism and drug resistance.

AR-C141990 hydrochloride is a selective inhibitor of monocarboxylate transporters (MCTs), specifically demonstrating pKi values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. This compound exhibits immunosuppressive properties and is utilized in research concerning graft versus host disease and metabolic regulation. Its ability to modulate lactate transport makes it a valuable tool for studying the role of MCTs in various biological processes.