Gap junction channel modulators

Gap junction channels physically connect adjacent cells, allowing the passage of ions and other small molecules between them and synchronizing cells both electrically and metabolically. Gap junction channels are composed of two hemichannels (connexons), which are formed from six connexin molecules, and allow the passive diffusion of a variety of molecules including nutrients, metabolites, ions and all known second messengers, facilitating electrical and biochemical coupling and enabling synchronized and rapid responses. Gap junction channels join virtually all cells in solid tissues and play an essential role in a wide range of physiological processes, including cardiac and smooth muscle contraction, regulation of neuronal excitability, epithelial electrolyte transport and keratinocyte differentiation. 

Isca Biochemicals now offer several important peptides for Gap junction channel research:

TAT-Gap19 is a connexin43 (Cx43) hemichannel blocker, with an IC50 of 7 μM and no significant affinity for gap junctions or Panx1 channels. TAT-Gap19 is derived from Gap19, a sequence present on the intracellular cytoplasmic loop domain of Cx43, linked to the HIV-derived TAT internalization sequence to promote membrane permeability, which also allows brain penetration. In mouse models of liver damage, TAT-Gap19 can protect against liver fibrosis accompanied by superoxide dismutase overactivation and reduces production of inflammatory proteins.

10Panx mimics a sequence (WRQAAFVDSY) in the second extracellular loop of Panx1 and is a panx-1 mimetic inhibitory peptide that blocks pannexin 1 gap junctions. 10Panx can inhibit Panx1 hemichannel mediated ATP release and inflammasome activation in astrocytes and macrophages and in vivo, pharmacological blockade of Panx1 hemichannels with 10Panx peptide attenuates the progression of acetaminophen induced hepatotoxicity, neuropathic pain and epilepsy.

Gap 26 is a connexin mimetic peptide corresponding to residues 63 - 75 of in the first extracellular loop of connexin 43, which inhibits currents carried by connexin43 hemichannels and gap junction channels. Gap 26 can accelerate wound healing and may have potential in the early treatment of spinal cord injury.

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All peptides are available from stock, in milligram to gram quantities. Please contact us with your requirements .