IndraLab

Statements

E-4031 inhibits KCNH2. 16 / 16
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"No effect of HERG channel blockage by E-4031 on cell proliferation."
22075718
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"However, neither E-4031 nor MK-499 at a concentration of 1 IIM blocked HERG current, even after the incubation of the oocytes for up to 4 hr in these drugs."
7736582
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"Because this drug is no longer available, we used the HERG blocker E-4031 to evaluate susceptibility to arrhythmia in control and A561P-UhiPS CMs."
26330336
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"Selective hERG channel blockade by E-4031 reduced proliferation in cancerous cell lines."
21850047
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"In the present experiments in HEK 293 cells, we found that E-4031 blocked HERG current in similarly low concentrations (IC 50 7.7 nM)."
9449325
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"Potentiation of late INa with ATX-II (anemonia sulcata toxin II) and E-4031 (selective blocker of the hERG channel) slowed the kinetics of action potential repolarization, impaired Ca 2+ homeostasis, increased contractility, and increased the manifestation of arrhythmia markers."
34103608
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"Use of HERG blockers including E-4031 and ergtoxin have still not been tested in vivo studies but do show a promising role in potential use with chemotherapeutic agents or in chemoresistant disease."
21190577
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"To determine the effect of E-4031 (an inhibitor of the KCNH2 channel) on beating frequency, videos were taken at the baseline (drug-free culture medium), with the drug, and following washout of the drug."
26785135
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"HERG current was blocked by low concentrations of E-4031 (IC50 7.7 nM), a value close to that reported for I (Kr) in native cardiac myocytes."
9449325
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"In line with previous findings that hERG channel blockage by E-4031 did not affect the K562 apoptosis [XREF_BIBR], our work showed scorpion toxin BmKKx2 could not cause the apoptosis by itself."
24386436
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"The selective hERG blocker E-4031 increased arrhythmogenicity in control cardiac cells and even more frequently in LQT2 cardiomyocytes (XREF_FIG)."
22052944
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"E-4031 is an inhibitor of the K V 11.1 (hERG), which mediates the repolarizing I Kr current in the action potential [XREF_BIBR]."
25956564
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"E-4031 could specifically block hERG1 channels when applied to cells maintained in standard extracellular saline solutions at concentrations of approximately 1 muM [26], so 1 muM E-4031 was therefore [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
19409379
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"E-4031 has also been shown to inhibit HERG channels [XREF_BIBR] while ergtoxin is a specific HERG blocker [XREF_BIBR]."
21392380
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"Experimental results XREF_BIBR shown in XREF_FIG (top) illustrate that E2 (1 nM) considerably increased the suppression of hERG by E-4031 (light gray line)."
20126530
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"The resulting dose response curve shows an increase in the IC 50 for E-4031 inhibition of hERG 1a/1b vs. 1a currents, from 6.2 +/- 1.1 nM to 25.6 +/- 4.3 nM, respectively (XREF_FIG)."
18776039