Piezo Channels

Piezo channels are mechanosensitive ion channels that mediate touch, hearing, proprioception, airway stretch sensation and blood pressure regulation. Piezo channel activation allows cation influx into cells resulting in membrane depolarization and activation of Ca2+-dependent signaling pathways.

Gene Data

Piezo Channel Modulators

Cat. No. Product Name / Activity
6568 Dooku 1
Reversibly blocks Yoda1 activity; does not affect constitutive Piezo1 activity

Piezo Channel Inhibitors

Cat. No. Product Name / Activity
4912 GsMTx4
Inhibits Piezo1 channels; also TRPC1 and TRPC6 blocker
7170 D-GsMTx4
Piezo2 and TRPC1/6 inhibitor; resistant to proteolytic digestion

Piezo Channel Activators

Cat. No. Product Name / Activity
6614 Jedi2
Piezo1 channel activator
5586 Yoda 1
Piezo1 channel activator
8051 Yoda 2
Piezo1 channel activator


Cat. No. Product Name / Activity
6545 OB-1
Stomatin-like protein-3 (STOML3) oligomerization inhibitor

The Piezo proteins comprise an evolutionarily conserved family of proteins that have no apparent sequence homology with other known ion channels. There are two Piezo genes, PIEZO1 and PIEZO2, encoding large transmembrane proteins of over 2500 amino acids. Piezo1 proteins assemble as trimeric complexes having at least 42 transmembrane segments and forming a central pore with three peripheral "wings". The C-terminal regions (residues 2189 - 2549) of the three assembled proteins form the central ion-conducting pore, which bears structural similarity to the pore of other trimeric ion channels (ASIC1 and P2X4), while the N-terminal non-pore containing regions (residues 1 - 2190) serve as the mechanotransduction modules. The peripheral regions, or wings, comprise extracellular "blade" domains, intracellular "beam"-like structures that anchor the blades to the pore, and "anchor" domains. The blade domains are highly flexible and it is thought that the ion channel is activated as a result of the peripheral regions acting as force sensors and transducers.

Piezo1 is involved in shear-stress sensing in blood vessels and is important in the development and function of the circulatory system. It is expressed in red blood cells and has a role in blood cell homeostasis. It is also implicated as a sensor of mechanical forces in endothelial, urothelial and epithelial cells. Piezo2 is expressed in sensory neurons and auditory hair cells and is key in touch sensation and proprioception, respiratory function and hearing.

External sources of pharmacological information for Piezo Channels :

    Piezo Channel Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Piezo1 Human PIEZO1 NM_014745 Q92508
    Mouse Piezo1 NM_001357349 E2JF22
    Rat Piezo1 NM_001077200 NP_001070668
    Piezo2 Human PIEZO2 NM_022068 Q9H5I5
    Mouse Piezo2 NM_001039485 Q8CD54
    Rat Piezo2 XM_225880 XP_225880