IndraLab

Statements

Rottlerin activates KCNH2. 9 / 10
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"Mallotoxin, an alkaloid isolated from the tree Mallotus phillippinensis, increases hERG1 current amplitude by causing a hyperpolarizing shift in the voltage dependence of channel activation, with a maximum shift of -24 mV at 10 muM and an EC 50 of 0.5 muM [XREF_BIBR]."
24721650
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"It should also be mentioned that the naturally occurring hERG1 channel agonist mallotoxin has been shown to activate hERG1 channels by a left-ward shift of the activation curve and a slowing of the de[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
19351523
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"16 , 24 , 30 , 58 Reports of the effects of agonist drug molecules exhibiting type 3 or 4 properties for the pharmacological management of diLQTS and cLQTS are by comparison scarce, 22 , 59 although they have been reported to increase the PRRP and shorten the QT interval but potentially to the point of triggering arrhythmia such as the type 3 hERG activator mallotoxin or type 4 PD118057."
35936037
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"In contrast, rottlerin inhibited PRAK and MAPKAP-K2, produced a substantial inhibition of JNK1α1, MSK1, PKA, PDK1, PKB/AKT, and GSK3β as well as non-kinase enzymes, including β-lactamase, α-chymotryps[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
26260013
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"Similar to KB130015, mallotoxin (MTx) activates the hERG1 channel by shifting its voltage dependence to the left and by accelerating activation."
20097192
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"In this study, we showed that both mallotoxin and NS1643 activated hERG current by 87% and 55% at 3muM, respectively."
18493243
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"In contrast to KB130015, mallotoxin slows down hERG1 deactivation, suggesting a different mode of action."
20097192
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"As expected, mallotoxin activated hERG current by 87% at 3muM, and NS1643 activated hERG current by 55% at 3muM."
18493243
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"Mallotoxin, which activated hERG current by 87% at 3muM in hERG transfected HEK293 cells, significantly shortened the QT interval, JT interval and APD and increased Tp-Te and rTp-Te and coronary flow at 0.1 muM."
18493243