para-Nitroblebbistatin, the Non-Cytotoxic and Photostable MyosinII Inhibitor

Blebbistatin, the best characterized myosinII-inhibitor, is commonly used to study the biological roles of various myosinII isoforms. Despite its popularity, the use of blebbistatin is greatly hindered by its blue-light sensitivity, resulting in phototoxicity and photoconversion of the molecule. Add...

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Bibliographic Details
Published inAngewandte Chemie International Edition Vol. 53; no. 31; pp. 8211 - 8215
Main Authors Kepiro, Miklós, Varkuti, Boglárka H, Vegner, László, Voros, Gergely, Hegyi, György, Varga, Máté, Malnasi-Csizmadia, András
Format Journal Article
LanguageEnglish
Published Weinheim Wiley Subscription Services, Inc 28.07.2014
EditionInternational ed. in English
Subjects
Analogue
Cellular
Cytotoxicity
Derivatives
Displays
Inhibition
Inhibitors
Parents
Side effects
Synthesis
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Summary:Blebbistatin, the best characterized myosinII-inhibitor, is commonly used to study the biological roles of various myosinII isoforms. Despite its popularity, the use of blebbistatin is greatly hindered by its blue-light sensitivity, resulting in phototoxicity and photoconversion of the molecule. Additionally, blebbistatin has serious cytotoxic side effects even in the absence of irradiation, which may easily lead to the misinterpretation of experimental results since the cytotoxicity-derived phenotype could be attributed to the inhibition of the myosinII function. Here we report the synthesis as well as the invitro and invivo characterization of a photostable, C15 nitro derivative of blebbistatin with unaffected myosinII inhibitory properties. Importantly, para-nitroblebbistatin is neither phototoxic nor cytotoxic, as shown by cellular and animal tests; therefore it can serve as an unrestricted and complete replacement of blebbistatin both invitro and invivo. [PUBLICATION ABSTRACT]
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ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201403540