Para-Nitroblebbistatin Explained
para-Nitroblebbistatin is a non-phototoxic, photostable myosin inhibitor with low fluorescence.[1] Its myosin inhibitory properties are very similar to those of blebbistatin.[2] [3]
Myosin specificity
| Species | Myosin type | IC50 |
|---|
| Rabbit | Skeletal muscle myosin S1 | 0.4 μM, 0.1 μM[4] [5] |
| Dictyostelium discoideum | Myosin II motor domain | 2.3 μM, 9 μM |
| Human | β-Cardiac myosin subfragment 1 | 13 μM[6] |
| Chicken | Heavy meromyosin fragment of skeletal muscle myosin | 0.4 μM |
| Pig (left ventricle) | cardiac myosin | 3.9 μM |
| Chicken (gizzard) | smooth muscle myosin S1 | 5.6 μM |
| Human (expressed in Sf9 cells) | non-muscle myosin 2A / B / C motor domains | 18 / 14 / 5 μM | |
Applications
para-Nitroblebbistatin has been successfully used in fluorescent imaging experiments involving myosin IIA-GFP expressing live dendritic cells[7] and synaptophysin-pHluorin expressing live neurons.[8]
Notes and References
- Képiró. Miklós. Várkuti. Boglárka H.. Végner. László. Vörös. Gergely. Hegyi. György. Varga. Máté. Málnási-Csizmadia. András. 2014-07-28. para-Nitroblebbistatin, the non-cytotoxic and photostable myosin II inhibitor. Angewandte Chemie International Edition in English. 53. 31. 8211–8215. 10.1002/anie.201403540. 1521-3773. 24954740.
- Rauscher. Anna Á.. Gyimesi. Máté. Kovács. Mihály. Málnási-Csizmadia. András. July 2018. Targeting Myosin by Blebbistatin Derivatives: Optimization and Pharmacological Potential. Trends in Biochemical Sciences. 43. 9. 700–713. 10.1016/j.tibs.2018.06.006. 30057142. 51864413 . 0968-0004.
- Roman. Bart I.. Verhasselt. Sigrid. Stevens. Christian V.. 2018-06-21. Medicinal Chemistry and Use of Myosin II Inhibitor (S)-Blebbistatin and Its Derivatives. Journal of Medicinal Chemistry. 61. 21. 9410–9428. en. 10.1021/acs.jmedchem.8b00503. 29878759. 46966833 . 0022-2623.
- Várkuti. Boglárka H.. Képiró. Miklós. Horváth. István Ádám. Végner. László. Ráti. Szilvia. Zsigmond. Áron. Hegyi. György. Lenkei. Zsolt. Varga. Máté. 2016-05-31. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Scientific Reports. 6. 26141. 10.1038/srep26141. 2045-2322. 4886532. 27241904. 2016NatSR...626141V.
- in press: Gyimesi et al Improved inhibitory and ADMET properties of blebbistatin derivatives indicate that blebbistatin scaffold is ideal for drug development targeting myosin-2 in Journal of Pharmacology and Experimental Therapies (2020)
- Tang. Wanjian. Blair. Cheavar A.. Walton. Shane D.. Málnási-Csizmadia. András. Campbell. Kenneth S.. Yengo. Christopher M.. 2016. Modulating Beta-Cardiac Myosin Function at the Molecular and Tissue Levels. Frontiers in Physiology. 7. 659. 10.3389/fphys.2016.00659. 1664-042X. 5220080. 28119616. free .
- Chabaud. Mélanie. Heuzé. Mélina L.. Bretou. Marine. Vargas. Pablo. Maiuri. Paolo. Solanes. Paola. Maurin. Mathieu. Terriac. Emmanuel. Le Berre. Maël. 2015-06-25. Cell migration and antigen capture are antagonistic processes coupled by myosin II in dendritic cells. Nature Communications. 6. 7526. 10.1038/ncomms8526. 2041-1723. 4491822. 26109323. 2015NatCo...6.7526C.
- Soykan. Tolga. Kaempf. Natalie. Sakaba. Takeshi. Vollweiter. Dennis. Goerdeler. Felix. Puchkov. Dmytro. Kononenko. Natalia L.. Haucke. Volker. Synaptic Vesicle Endocytosis Occurs on Multiple Timescales and Is Mediated by Formin-Dependent Actin Assembly. Neuron. 93. 4. 854–866.e4. 10.1016/j.neuron.2017.02.011. 28231467. 2017. free.
