Home / Monocarboxylate Transporter Inhibitors / AR-C155858

AR-C155858

Catalog #: 4960
5 Citations 1 Review Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4960/1
AR-C155858 | CAS No. 496791-37-8 | Monocarboxylate Transporter Inhibitors
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Description: MCT1 and MCT2 inhibitor; inhibits glycolysis in cancer cells

Chemical Name: 6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione

Purity: ≥98%

Product Details
Citations (5)
Supplemental Products
Reviews (1)
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
461.53
Formula:
C21H27N5O5S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
496791-37-8

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca UK Limited

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Citations for AR-C155858

The citations listed below are publications that use Tocris products. Selected citations for AR-C155858 include:

5 Citations: Showing 1 - 5

  1. Lactate and pyruvate promote oxidative stress resistance through hormetic ROS signaling.
    Authors: Tauffenberger Et al.
    Cell Death Dis  2019;10:653
  2. The Glia-Neuron Lactate Shuttle and Elevated ROS Promote Lipid Synthesis in Neurons and Lipid Droplet Accumulation in Glia via APOE/D.
    Authors: Liu Et al.
    Cell Metab  2017;26:719
  3. Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake.
    Authors: Diaz-Garcia Et al.
    Cell Metab  2017;26:361
  4. Hypoxia-induced carbonic anhydrase IX facilitates lactate flux in human breast cancer cells by non-catalytic function.
    Authors: Jamali Et al.
    Sci Rep  2015;5:13605
  5. Lactate Regulates Metabolic and Pro-inflammatory Circuits in Control of T Cell Migration and Effector Functions.
    Authors: Haas Et al.
    Nat Commun  2015;13:e1002202

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VersaClone cDNA Plasmids

Human MCT1/SLC16A1 (NP_001159968) VersaClone cDNA

RDC0533

Reviews for AR-C155858

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Blocking MCT activity in small intestine
By Tauseef Ahmad on 02/12/2018

To transiently block uptake capacity of MCT receptors in small intestine of in an ex vivo rodent model

Only partial blockage achieved at selected concentration

Blocking MCT activity in small intestine 4960
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