You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!Submit Review
Biological Activity for AR-C155858
AR-C155858 is an inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and <10 nM respectively). Exhibits no activity at MCT4. Blocks proliferation of Raji lymphoma cells in vitro. Inhibits glycolysis and glutathione synthesis in cancer cells.
Sold for research purposes under agreement from AstraZeneca UK Limited
Technical Data for AR-C155858
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AR-C155858
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for AR-C155858
The following data is based on the product molecular weight 461.53. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.17 mL||10.83 mL||21.67 mL|
|5 mM||0.43 mL||2.17 mL||4.33 mL|
|10 mM||0.22 mL||1.08 mL||2.17 mL|
|50 mM||0.04 mL||0.22 mL||0.43 mL|
References for AR-C155858
References are publications that support the biological activity of the product.
Ovens et al (2010) The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem.J. 431 217 PMID: 20695846
Ovens et al (2010) AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem.J. 425 523 PMID: 19929853
Doherty et al (2014) Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis. Cancer Res. 74 908 PMID: 24285728
If you know of a relevant reference for AR-C155858, please let us know.
View Related Products by Product Action
Keywords: AR-C155858, AR-C155858 supplier, monocarboxylate, transporters, MCT1, MCT2, inhibitors, inhibits, Monocarboxylate, Transporters, 4960, Tocris Bioscience
18 Citations for AR-C155858
Citations are publications that use Tocris products. Selected citations for AR-C155858 include:
Adam J et al (2023) High glucose promotes regulatory T cell differentiation. PLoS One 18 e0280916 PMID: 36730267
Sandra L et al (2023) Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix. iScience 26 105965 PMID: 36824274
Diaz-Garcia et al (2017) Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake. Cell Metab 26 361 PMID: 28768175
Steven A et al (2017) Type 2 Diabetes Variants Disrupt Function of SLC16A11 through Two Distinct Mechanisms. Cell 170 199-212.e20 PMID: 28666119
Bruce P et al (2018) Glucose and lactate as metabolic constraints on presynaptic transmission at an excitatory synapse. J Physiol 596 1699-1721 PMID: 29430661
Jeffrey D et al (2021) MCT1 Deletion in Oligodendrocyte Lineage Cells Causes Late-Onset Hypomyelination and Axonal Degeneration. Cell Rep 34 108610 PMID: 33440165
Atsushi et al (2021) Protein lactylation induced by neural excitation. Cell Rep 37 109820 PMID: 34644564
Maria Letizia et al (2019) Cancer-associated fibroblasts promote prostate cancer malignancy via metabolic rewiring and mitochondrial transfer. Oncogene 38 5339-5355 PMID: 30936458
Liu et al (2017) The Glia-Neuron Lactate Shuttle and Elevated ROS Promote Lipid Synthesis in Neurons and Lipid Droplet Accumulation in Glia via APOE/D. Cell Metab 26 719 PMID: 28965825
Haas et al (2015) Lactate Regulates Metabolic and Pro-inflammatory Circuits in Control of T Cell Migration and Effector Functions. Nat Commun 13 e1002202 PMID: 26181372
Jamali et al (2015) Hypoxia-induced carbonic anhydrase IX facilitates lactate flux in human breast cancer cells by non-catalytic function. Sci Rep 5 13605 PMID: 26337752
Wiktoria et al (2022) Autoregulation of H+/lactate efflux prevents monocarboxylate transport (MCT) inhibitors from reducing glycolytic lactic acid production. Br J Cancer 127 1365-1377 PMID: 35840734
Matteo et al (2022) Lactate Rewires Lipid Metabolism and Sustains a Metabolic-Epigenetic Axis in Prostate Cancer. Cancer Res 82 1267-1282 PMID: 35135811
Tauffenberger et al (2019) Lactate and pyruvate promote oxidative stress resistance through hormetic ROS signaling. Cell Death Dis 10 653 PMID: 31506428
Holger M et al (2020) CAIX forms a transport metabolon with monocarboxylate transporters in human breast cancer cells. Oncogene 39 1710-1723 PMID: 31723238
Keit Men et al (2020) A glycolytic shift in Schwann cells supports injured axons. Nat Neurosci 23 1215-1228 PMID: 32807950
Emy et al (2020) Defective Mitochondrial Pyruvate Flux Affects Cell Bioenergetics in Alzheimer's Disease-Related Models. Cell Rep 30 2332-2348.e10 PMID: 32075767
Charles et al (2020) Impairment of Glycolysis-Derived l-Serine Production in Astrocytes Contributes to Cognitive Deficits in Alzheimer's Disease. Cell Metab 31 503-517.e8 PMID: 32130882
Do you know of a great paper that uses AR-C155858 from Tocris? Please let us know.
Reviews for AR-C155858
There are currently no reviews for this product. Be the first to review AR-C155858 and earn rewards!
Have you used AR-C155858?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Metabolism Research Product GuideNew
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Tricarboxylic Acid Cycle
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.