AR-C155858 (CAS 496791-37-8)
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AR-C155858 is a compound of interest within the biochemical research community due to its role as an inhibitor of monocarboxylate transporters (MCTs). This specificity makes it useful for probing the metabolic shifts in cells that rely heavily on glycolysis and lactate export, such as in various models of metabolic reprogramming. Researchers utilize AR-C155858 to investigate the transport mechanisms of monocarboxylates across cellular membranes and its impact on cellular metabolism and energy homeostasis. The compound′s ability to inhibit MCTs has also made it instrumental in studies focusing on metabolic flux and the adaptation of cells to hypoxic conditions. Additionally, AR-C155858 is applied in metabolic engineering to understand how blocking lactate export can redirect cellular pathways, potentially leading to the accumulation of desired metabolites, which is of particular interest in the field of industrial biotechnology.
AR-C155858 (CAS 496791-37-8) References
- AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. | Ovens, MJ., et al. 2010. Biochem J. 425: 523-30. PMID: 19929853
- The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. | Ovens, MJ., et al. 2010. Biochem J. 431: 217-25. PMID: 20695846
- Identification of key binding site residues of MCT1 for AR-C155858 reveals the molecular basis of its isoform selectivity. | Nancolas, B., et al. 2015. Biochem J. 466: 177-88. PMID: 25437897
- A Novel Monocarboxylate Transporter Inhibitor as a Potential Treatment Strategy for γ-Hydroxybutyric Acid Overdose. | Vijay, N., et al. 2015. Pharm Res. 32: 1894-906. PMID: 25480120
- Identification of key binding site residues of MCT1 for AR-C155858 reveals the molecular basis of its isoform selectivity. | Nancolas, B., et al. 2015. Biochem J. 467: 192. PMID: 25793420
- Glucose-dependent growth arrest of leukemia cells by MCT1 inhibition: Feeding Warburg's sweet tooth and blocking acid export as an anticancer strategy. | Pivovarova, AI. and MacGregor, GG. 2018. Biomed Pharmacother. 98: 173-179. PMID: 29253765
- In Vitro and In Vivo Efficacy of the Monocarboxylate Transporter 1 Inhibitor AR-C155858 in the Murine 4T1 Breast Cancer Tumor Model. | Guan, X., et al. 2018. AAPS J. 21: 3. PMID: 30397860
- Cellular Uptake of MCT1 Inhibitors AR-C155858 and AZD3965 and Their Effects on MCT-Mediated Transport of L-Lactate in Murine 4T1 Breast Tumor Cancer Cells. | Guan, X., et al. 2019. AAPS J. 21: 13. PMID: 30617815
- Targeted sensitization of tumor cells for radiation through monocarboxylate transporters 1 and 4 inhibition in vitro. | Brandstetter, G., et al. 2021. Clin Oral Investig. 25: 295-310. PMID: 32495222
- Targeting Lactate Metabolism by Inhibiting MCT1 or MCT4 Impairs Leukemic Cell Proliferation, Induces Two Different Related Death-Pathways and Increases Chemotherapeutic Sensitivity of Acute Myeloid Leukemia Cells. | Saulle, E., et al. 2020. Front Oncol. 10: 621458. PMID: 33614502
- γ-Hydroxybutyric Acid-Ethanol Drug-Drug Interaction: Reversal of Toxicity with Monocarboxylate Transporter 1 Inhibitors. | Rodriguez-Cruz, V. and Morris, ME. 2021. J Pharmacol Exp Ther. 378: 42-50. PMID: 33963018
- MCT1 Is a New Prognostic Biomarker and Its Therapeutic Inhibition Boosts Response to Temozolomide in Human Glioblastoma. | Miranda-Gonçalves, V., et al. 2021. Cancers (Basel). 13: PMID: 34298681
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AR-C155858, 1 mg | sc-480179 | 1 mg | $369.00 | |||
AR-C155858, 5 mg | sc-480179A | 5 mg | $779.00 | |||
AR-C155858, 10 mg | sc-480179B | 10 mg | $1306.00 | |||
AR-C155858, 50 mg | sc-480179C | 50 mg | $3818.00 |