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Description: Piezo1 channel activator
Chemical Name: 2-[5-[[(2,6-Dichlorophenyl)methyl]thio]-1,3,4-thiadiazol-2-yl]pyrazine
Purity: ≥99% (HPLC)
Biological Activity for Yoda 1
Yoda 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.
Compound Libraries for Yoda 1
Yoda 1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Yoda 1
| M. Wt | 355.27 |
| Formula | C13H8Cl2N4S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 448947-81-7 |
| PubChem ID | 2746822 |
| InChI Key | BQNXBSYSQXSXPT-UHFFFAOYSA-N |
| Smiles | ClC1=C(CSC2=NN=C(C3=NC=CN=C3)S2)C(Cl)=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Yoda 1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.11 | 20 |
Preparing Stock Solutions for Yoda 1
The following data is based on the product molecular weight 355.27. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 14.07 mL | 70.37 mL | 140.74 mL |
| 1 mM | 2.81 mL | 14.07 mL | 28.15 mL |
| 2 mM | 1.41 mL | 7.04 mL | 14.07 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.81 mL |
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Product Datasheets for Yoda 1
References for Yoda 1
References are publications that support the biological activity of the product.
Syeda et al (2015) Chemical activation of the mechanotransduction channel Piezo1. ELife 4 e07369 PMID: 26001275
Mikhailov et al (2019) Mechanosensitive meningeal nociception via Piezo channels: Implications for pulsatile pain in migraine? Neuropharmacology 149 113 PMID: 30768945
Jetta et al (2019) Shear stress-induced nuclear shrinkage through activation of Piezo1 channels in epithelial cells. J.Cell Sci. 132 jcs226076 PMID: 31076516
Cahalan et al (2015) Piezo1 links mechanical forces to red blood cell volume. Elife. 4 e07370 PMID: 26001274
If you know of a relevant reference for Yoda 1, please let us know.
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Keywords: Yoda 1, Yoda 1 supplier, Yoda1, Piezo1, calcium, channels, activators, sensitizers, sensitizes, Ca2+, currents, mechanotransduction, Piezo, Channels, 5586, Tocris Bioscience
38 Citations for Yoda 1
Citations are publications that use Tocris products. Selected citations for Yoda 1 include:
Yaganoglu et al (2023) Highly specific and non-invasive imaging of Piezo1-dependent activity across scales using GenEPi. Nat Commun 14 4352 PMID: 37468521
Cynthia A et al (2023) Matrix stiffness induces epithelial-to-mesenchymal transition via Piezo1-regulated calcium flux in prostate cancer cells. iScience 26 106275 PMID: 36950111
Ping et al (2023) Piezo1 channel activation stimulates ATP production through enhancing mitochondrial respiration and glycolysis in vascular endothelial cells. Br J Pharmacol 180 1862-1877 PMID: 36740831
Ilkan et al (2017) Evidence for shear-mediated Ca2+ entry through mechanosensitive cation channels in human platelets and a megakaryocytic cell line. J Biol Chem 292 9204 PMID: 28416610
Chubinskiy-Nadezhdin et al (2019) Agonist-induced Piezo1 activation suppresses migration of transformed fibroblasts. Biochem Biophys Res Commun. 514 173 PMID: 31029419
Ophir D et al (2021) Inflation-collapse dynamics drive patterning and morphogenesis in intestinal organoids. Cell Stem Cell 28 1516-1532.e14 PMID: 33915079
Udo et al (2021) Piezo1 Inactivation in Chondrocytes Impairs Trabecular Bone Formation. J Bone Miner Res 36 369-384 PMID: 33180356
Adler L et al (2021) Mammary mechanobiology - investigating roles for mechanically activated ion channels in lactation and involution. J Cell Sci 134 PMID: 33262312
Ping et al (2021) TLR4 signalling via Piezo1 engages and enhances the macrophage mediated host response during bacterial infection. Nat Commun 12 3519 PMID: 34112781
Yuri et al (2021) Selective Chemical Activation of Piezo1 in Leukemia Cell Membrane: Single Channel Analysis. Int J Mol Sci 22 PMID: 34360605
Chii Jou et al (2021) Cell fate coordinates mechano-osmotic forces in intestinal crypt formation. Nat Cell Biol 23 733-744 PMID: 34155381
Yu et al (2021) A role of PIEZO1 in iron metabolism in mice and humans. Cell 184 969-982.e13 PMID: 33571427
James et al (2022) Sonogenetic control of mammalian cells using exogenous Transient Receptor Potential A1 channels. Nat Commun 13 600 PMID: 35140203
James D et al (2022) Flow-Induced Secretion of Endothelial Heparanase Regulates Cardiac Lipoprotein Lipase and Changes Following Diabetes. J Am Heart Assoc 11 e027958 PMID: 36416172
Yan et al (2022) Mechanosensitive piezo1 calcium channel activates connexin 43 hemichannels through PI3K signaling pathway in bone. Cell Biosci 12 191 PMID: 36457052
Alla et al (2022) Store-Operated Ca2+ Entry Contributes to Piezo1-Induced Ca2+ Increase in Human Endometrial Stem Cells. Int J Mol Sci 23 PMID: 35409116
Steven R et al (2022) Piezo1-mediated stellate cell activation causes pressure-induced pancreatic fibrosis in mice. JCI Insight 7 PMID: 35451372
Rupalatha et al (2022) Mechanical Load and Piezo1 Channel Regulated Myosin II Activity in Mouse Lenses. Int J Mol Sci 23 PMID: 35563101
Katja M et al (2022) Microglial amyloid beta clearance is driven by PIEZO1 channels. J Neuroinflammation 19 147 PMID: 35706029
Ting et al (2022) Mechanosensation by endothelial PIEZO1 is required for leukocyte diapedesis. Blood 140 171-183 PMID: 35443048
Ilona et al (2022) Mechanoreceptor Piezo1 Is Downregulated in Multiple Sclerosis Brain and Is Involved in the Maturation and Migration of Oligodendrocytes in vitro. Front Cell Neurosci 16 914985 PMID: 35722613
Stephanie W et al (2022) PIEZO1 mechanoreceptor activation reduces adipogenesis in perivascular adipose tissue preadipocytes. Front Endocrinol (Lausanne) 13 995499 PMID: 36120469
Willem-Jan et al (2022) A mechanical G2 checkpoint controls epithelial cell division through E-cadherin-mediated regulation of Wee1-Cdk1. Cell Rep 41 111475 PMID: 36223752
Yuan et al (2022) Inhibition of chemically and mechanically activated Piezo1 channels as a mechanism for ameliorating atherosclerosis with salvianolic acid B. Br J Pharmacol 179 3778-3814 PMID: 35194776
Yannick et al (2022) Piezo channels contribute to the regulation of myelination in Schwann cells. Glia 70 2276-2289 PMID: 35903933
Dela Paz (2018) Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun 497 220 PMID: 29428723
Tsuchiya (2018) Cell surface flip-flop of phosphatidylserine is critical for PIEZO1-mediated myotube formation. Nat Commun 9 2049 PMID: 29799007
Bo et al (2020) Piezo1/2 mediate mechanotransduction essential for bone formation through concerted activation of NFAT-YAP1-β-catenin. Elife 9 PMID: 32186512
Rodger A et al (2020) Piezo1 acts upstream of TRPV4 to induce pathological changes in endothelial cells due to shear stress. J Biol Chem 296 100171 PMID: 33298523
Jian et al (2020) Sphingomyelinase Disables Inactivation in Endogenous PIEZO1 Channels. Cell Rep 33 108225 PMID: 33027663
T Simon et al (2020) Shear stress activates ADAM10 sheddase to regulate Notch1 via the Piezo1 force sensor in endothelial cells. Elife 9 PMID: 32484440
Erin J et al (2020) Caenorhabditis elegans PIEZO channel coordinates multiple reproductive tissues to govern ovulation. Elife 9 PMID: 32490809
Stephen J et al (2020) TRPV4 channel opening mediates pressure-induced pancreatitis initiated by Piezo1 activation. J Clin Invest 130 2527-2541 PMID: 31999644
Adler L et al (2020) Mammary mechanobiology: Investigating roles for mechanically-activated ion channels in lactation and involution. J Cell Sci PMID: 34005376
Qi et al (2020) Piezo1-Mediated Ca2+ Activities Regulate Brain Vascular Pathfinding during Development. Neuron 108 180-192.e5 PMID: 32827455
Stuart et al (2020) Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia 68 356-375 PMID: 31596529
Maria et al (2020) Piezo1 regulates calcium oscillations and cytokine release from astrocytes. Glia 68 145-160 PMID: 31433095
Romac et al (2018) Piezo1 is a mechanically activated ion channel and mediates pressure induced pancreatitis. Nat Commun 9 1715 PMID: 29712913
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Reviews for Yoda 1
Average Rating: 5 (Based on 2 Reviews.)
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Stimulation of Piezo1 activity.
By
Vladislav Chubinskiy-Nadezhdin on 08/16/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: 3T3B-SV40
Used in patch-clamp, cell migration assay (1-30 uM)
A potent piezo1 receptor activator.
By
Hyun Choi on 02/21/2018
Assay Type: Ex Vivo
Species: Rat
We used to stimulate piezo1 receptor at around 1-10microM