Chemical Name: 2-[5-[[(2,6-Dichlorophenyl)methyl]thio]-1,3,4-thiadiazol-2-yl]pyrazine
Biological ActivityYoda 1 is a selective activator of mouse and human mechanosensitive channel piezo1. In HEK cells, Yoda 1 slows the inactivation phase of transient currents, sensitizes Piezo1 to activation by pressure, and partially activates channels in the absence of external pressure. In MDCK cells, Yoda 1 induces Ca2+-dependent chromatin hypercondensation and alters Ca2+-dependent myosin contractility, leading to nuclear shrinkage in cells. In red blood cells from sickle cell anemia (SCA) patients, Yoda 1 increases intracellular Ca2+ and phosphatidylserine exposure, which leads to KCa3.1 channel mediated Ca2+ influx and K+ and water efflux, causing shrinkage of the cells.
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Chemical activation of the mechanotransduction channel Piezo1.
Syeda et al.
Mechanosensitive meningeal nociception via Piezo channels: Implications for pulsatile pain in migraine?
Mikhailov et al.
Citations for Yoda 1
The citations listed below are publications that use Tocris products. Selected citations for Yoda 1 include:
5 Citations: Showing 1 - 5
Agonist-induced Piezo1 activation suppresses migration of transformed fibroblasts.
Authors: Chubinskiy-Nadezhdin Et al.
Biochem Biophys Res Commun. 2019;514:173
Piezo1 is a mechanically activated ion channel and mediates pressure induced pancreatitis.
Authors: Romac Et al.
Nat Commun 2018;9:1715
Cell surface flip-flop of phosphatidylserine is critical for PIEZO1-mediated myotube formation.
Nat Commun 2018;9(1):2049
Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation.
Authors: Dela Paz
Biochem Biophys Res Commun 2018;497(1):220
Evidence for shear-mediated Ca2+ entry through mechanosensitive cation channels in human platelets and a megakaryocytic cell line.
Authors: Ilkan Et al.
J Biol Chem 2017;292:9204
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