1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. Piezo Channel

Piezo Channel

Piezo channels are the trimeric mechanosensitive ion channels that open in response to mechanical stimuli such as shear stress and membrane stretch, allowing positively charged ions, including calcium, to flow into the cell. It is speculated that extracellular mechanical stimuli can be converted into tension from lipid molecules in the cell membrane to activate the Piezo channels. The intracellular beam might transmit tension from lipid molecules from the distal blade to the central pore module by means of a lever principle, which opens the central pore for ion-conducting. Most vertebrates have two channel isoforms, Piezo1 and Piezo2. Piezo1 and Piezo2 are involved in various mechanotransduction pathways, including touch sensation, proprioception, nociception, vascular development, and breathing. In humans, gain-of-function mutations in Piezo1 are linked to dehydrated hereditary stomatocytosis (DHS). Loss-of-function mutations in Piezo1 and Piezo2 are linked to congenital lymphatic dysplasia14 and defective touch perception and proprioception.

Piezo Channel Related Products (9):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18723
    Yoda 1
    Agonist 99.98%
    Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
    Yoda 1
  • HY-P1410
    GsMTx4
    Inhibitor 99.80%
    GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
    GsMTx4
  • HY-126010
    Dooku1
    Antagonist 99.89%
    Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research.
    Dooku1
  • HY-P1410A
    GsMTx4 TFA
    Inhibitor 99.80%
    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
    GsMTx4 TFA
  • HY-P1410C
    D-GsMTx4 TFA
    Inhibitor 99.89%
    D-GsMTx4 TFA, a spider peptide, is the D-enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA can be used for research of mechanical stress.
    D-GsMTx4 TFA
  • HY-162501
    Yaddle1
    Agonist 99.14%
    Yaddle1 (compound 34) a novel Piezo1 agonist, and induces Ca2+ influx in human CD4+ T cell. Yaddle1 can be used for study of vaccine adjuvant.
    Yaddle1
  • HY-169332
    Piezo1 agonist 1-d2
    Agonist
    Piezo1 agonist 1-d2 (Compound 12a) is an agonist for Piezo1 with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates the Ca2+-related ERK signaling pathway, and thus promotes the osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs). Piezo1 agonist 1-d2 ameliorates disuse osteoporosis in the hindlimb-unloading (HU) rat model.
    Piezo1 agonist 1-d<sub>2</sub>
  • HY-131018
    Jedi2
    99.93%
    Jedi2 is a Piezo1 activator, but not a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770??μM.
    Jedi2
  • HY-P1410B
    D-GsMTx4
    Inhibitor 99.44%
    D-GsMTx4, a spider peptide, is the D-enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 can be used for research of mechanical stress.
    D-GsMTx4