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E-4031

A Blocker of KV11.1 (hERG) K+ Channels

Cat #: E-500
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 510.5
    Purity: >98%
    Effective concentration 100 nM - 1 μM.
    Structure
    Chemical name (1-[2-(6-Methyl-2-pyridyl)ethyl]-4-(4-methylsulfonyl-aminobenzoyl)piperidine).
    Molecular formula C21H27N3O3S•2HCl•2H2O.
    CAS No.: 113559-13-0
    Activity E-4031 is a methsnesulfonanilide class III antiarrhythmic agent. It specifically blocks hERG (KV11.1) voltage-gated K+ channel current in heterologous systems1,2, cardiac cells3 and cardiac preparations4.
    References-Activity
    1. Spector, P.S. et al. (1996) Circ. Res. 78, 499.
    2. Zhou, Z. et al. (1998) Biophys. J. 74, 230.
    3. Sanguinetti, M.C. and Jurkiewicz, N.K. (1990) J. Gen. Physiol. 96, 195.
    4. Wettwer, E. et al. (1991) J. Cardiovasc. Pharmacol. 17, 480.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs E-4031 inhibits HERG K+ currents heterologously expressed in HEK-293 cells.
      Alomone Labs E-4031 inhibits HERG K+ currents heterologously expressed in HEK-293 cells.
      Top: Traces of KV11.1 currents elicited every 5 seconds from a holding potential of -100 mV, by a compound test pulse (250 ms at +20 mV followed by 250 ms at -40 mV), before (blue) and during (green) application of 1 μM E-4031 (#E-500). Bottom: Dose-response relationship describing the inhibition of KV11.1 currents by increasing concentrations of E-4031. IC50 was at about 500 nM. Data and SD values for n = 4-9 are given.
    References - Scientific background
    1. Spector, P.S. et al. (1996) Circ Res. 78, 499.
    2. Zhou, Z. et al. (1998) Biophys. J. 74, 230.
    3. Sanguinetti, M.C. and Jurkiewicz, N.K. (1990) J. Gen Physiol. 96, 195.
    4. Wettwer, E. et al. (1991) J. Cardiovasc. Pharmacol. 17, 480.
    5. Anderson, C.L. et al. (2006) Circulation 113, 365.
    6. Cherubini, A. et al. (2005) Mol. Biol. Cell 16, 2972.
    7. Kim, I. et al. (2005) J. Appl. Physiol. 98, 1469.
    8. Liu, J.H. et al. (2003) Development 130, 3437.
    Scientific background E-4031 is a methanesulfonanilide class III antiarrhythmic agent known to inhibit KV11.1 (hERG) channels. Sub-micromolar concentration of E-4031, selectively blocks Kv11.1 channels, either in heterologous systems,1,2 cardiac cells3 and cardiac preparations.4 E-4031 was shown to rescue the functional expression of mutated (LQ2) KV11.1 channels in HEK cells.5 E-4031 (40 µM) treatment also prevented FAK phosphorylation and Rac1 activity (only in HEK cells expressing the KV11.1 subunit).6 In rat carotid chemoreceptor cells, 1 µM E-4031 inhibited the KV current, to a larger extent in postnatal cells, establishing the developmental disappearance of KV11.1 channels and their contribution to the response to hypoxia.7 E-4031 (1 µM) accelerated myoblast fusion, probably by blocking KV11.1 channels that leads to depolarization.8
    Target KV11.1 K+ channels
    Lyophilized Powder
    Image & Title E-4031
    Alomone Labs E-4031 blocks hERG channels in HEK 293 transfected cells.Current vs voltage (I-V) curve before and after application of 1 µM E-4031 (#E-500) to cells.Adapted from Schlichter, L.C. et al. (2014) PLoS ONE 9, e90024. with permission of PLoS.
    Last update: 24/01/2021

    E-4031 (#E-500) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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    Scientific Background

    Citations

    Citations
    Product citations
    1. Altomare, C. et al. (2016) Europace 18, iv67.
    2. Schlichter, L.C. et al. (2014) PLoS ONE 9, e90024.
    3. Wondergem, R. et al. (2012) Am. J. Physiol. 303, C825.

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    Shipping and Ordering information

    Resources

    K+ Channels in Cardiomyocytes

    The Involvement of Ion Channels in Cell Proliferation

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