1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter

AR-C155858 

Cat. No.: HY-13248 Purity: 95.09% ee.: 99.30%
Data Sheet SDS Handling Instructions

AR-C155858 is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.

For research use only. We do not sell to patients.
AR-C155858 Chemical Structure

AR-C155858 Chemical Structure

CAS No. : 496791-37-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO $315 In-stock
1 mg $110 In-stock
5 mg $310 In-stock
10 mg $520 In-stock
50 mg $1520 In-stock
100 mg   Get quote  
200 mg   Get quote  

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    AR-C155858 purchased from MCE. Usage Cited in: Oncotarget. 2014 Nov 30;5(22):11029-37.

    The MCT1/2 inhibitor AR-C155858 significantly reduces mammosphere formation in MDA-MB-231 cells. Note that AR-C155858 also effectively reduces mammosphere formation in this cellular context, with an IC50 of ~1-2 μM. The vehicle-alone control is normalized to one.

    AR-C155858 purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C116-26.

    Inhibition of pyruvate transport in HEK293 cells. Summary of 24 cells in three separate experiments.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AR-C155858 is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and < 10 nM, respectively), and exhibits no activity at MCT4.

    IC50 & Target

    Ki: 2.3 nM (MCT1), 10 nM (MCT2)

    In Vitro

    AR-C155858 (10 nM-100 nM) inhibits MCT1/MCT2 C-terminal chimaeras[1]. AR-C155858 inhibits MCT2, and the 70% inhibition seen at 10 nM is followed by a gradually increasing inhibition which can only be explained by a Ki value of significantly less than 10 nM. AR-C155858 inhibits MCT1 expressed in Xenopus oocytes in a time- and concentration-dependent manner[2].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.1667 mL 10.8335 mL 21.6671 mL
    5 mM 0.4333 mL 2.1667 mL 4.3334 mL
    10 mM 0.2167 mL 1.0834 mL 2.1667 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    MCT kinetic assays are performed by monitoring intracellular pH with H+-sensitive dye BCECF or by determining the uptake of l-[14C]lactate (7.4 MBq/mL). The uptake buffer containes 75 mM NaCl, 2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Tris/Hepes (pH 7.4). AR-C155858 inhibitor titrations are performed at pH 6 with oocytes preincubated for 45 min in a different uptake buffer (75 mM NaCl, 2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Mes, pH 6) containing the required concentration of AR-C155858 prior to measuring the uptake of l-[14C]lactate (0.5 mM). Unless stated otherwise, uptake is determined over 2.5 min for all MCT constructs except for MCT2trn with or without embigin and MCT2/1 with or without embigin, where 5 and 10 min are used respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    AR-C155858 is dissolved in DMSO.

    The erythrocytes (5% haematocrit) are pre-incubated for 1 h at room temperature (22°C) with or without AR-C155858 at the required concentration before assaying transport of l-lactate (10 mM) at 6°C. Initial rates of transport are calculated by first-order regression analysis of the time course of pH change and converted into nmol of H+/min by determining the pH change induced by small additions of standardized NaOH. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    461.53

    Formula

    C₂₁H₂₇N₅O₅S

    CAS No.

    496791-37-8

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    AR-C155858 is prepared as a 2.5 mg/mL solution in 10% cyclodextrin in normal saline[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    AR-C155858
    Cat. No.:
    HY-13248
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