AR-C155858

AR-C155858 is a chemical compound known for its role as an inhibitor of the monocarboxylate transporter (MCT) family, specifically targeting MCT1 and MCT2. These transporters are integral membrane proteins that facilitate the transport of lactate, pyruvate, and other monocarboxylates across the plasma membrane.

Mechanism of Action

AR-C155858 functions by binding to the MCT1 and MCT2 transporters, thereby inhibiting their activity. This inhibition prevents the transport of lactate and pyruvate, which are crucial substrates in cellular metabolism, particularly under anaerobic conditions. By blocking these transporters, AR-C155858 can alter cellular metabolism, which has implications in various physiological and pathological processes.

Pharmacological Significance

The inhibition of MCT1 and MCT2 by AR-C155858 has been studied in the context of cancer metabolism. Tumor cells often rely on glycolysis followed by lactate export to sustain their rapid growth, a phenomenon known as the Warburg effect. By inhibiting lactate transport, AR-C155858 can disrupt the metabolic flexibility of cancer cells, potentially leading to reduced tumor growth and viability.

Research and Development

AR-C155858 has been utilized in various research studies to explore the role of monocarboxylate transporters in health and disease. Its ability to selectively inhibit MCT1 and MCT2 makes it a valuable tool in the study of metabolic pathways and their implications in diseases such as cancer, diabetes, and cardiovascular disorders.

Potential Therapeutic Applications

While primarily a research tool, the potential therapeutic applications of AR-C155858 are being explored. Its role in modulating cellular metabolism suggests possible uses in cancer therapy, where metabolic reprogramming is a hallmark of disease progression.

Safety and Toxicology

As with many experimental compounds, the safety and toxicological profile of AR-C155858 is not fully established. Further studies are required to determine its safety in clinical settings.

Also see

• Monocarboxylate transporter
• Cancer metabolism
• Warburg effect
• Glycolysis