connexin

Gap19 is a peptide that corresponds to a sequence on the cytoplasmic loop (CL) of Cx43.

Connexin mimetic peptide 40GAP27, corresponding to the GAP27 domain of the second extracellular loop of the dominant vascular connexin (Cx40), designated as 40Gap27, is a biologically active peptide utilized to study the pathways by which oxidant stress hinders gap junction communication. Administered 40Gap27 attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.

Connexin mimetic peptide 40,37GAP26, a biologically active peptide, matches the GAP26 domain of the extracellular loop of major vascular connexins Cx37 and Cx40, referred to as 37,40Gap26 based on Cx homology. It has been utilized to examine gap junctions' involvement in propagating endothelial hyperpolarizations induced by cyclopiazonic acid (CPA) in the rodent iliac artery wall. Abundant gap junction plaques comprising Cx37 and Cx40 are present in the endothelium, and the peptide exerts inhibitory actions on subintimal hyperpolarization.

Rotigaptide is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress.

Trovafloxacin mesylate is a fluoroquinolone antibiotic and a dual inhibitor of DNA gyrase and topoisomerase IV, as well as a selective inhibitor of the Pannexin 1 channel (IC50 = 4 μM). With oral bioactivity and cell permeability, Trovafloxacin does not inhibit connexin 43 or PANX2, and is used for antibacterial therapy.

Cx43 HC-IN-1 (Compound D4) is a selective, orally active inhibitor of connexin hemichannels (Cx43 HC). It effectively suppresses hemichannel activity mediated by Cx43/Cx45 in denervated skeletal muscle fibers, significantly enhancing neuronal reinnervation of muscle fibers. By inhibiting hemichannels in brain glial cells, Cx43 HC-IN-1 reduces neuroinflammation and neuronal hyperexcitability, alleviating seizures in mice. It is applicable for research on epilepsy and muscular disorders.

PQ1, as an enhancer of gap junction in SW480 human colorectal cancer cells can act by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.

PQ1 Succinate, a gap junction enhancer, acts by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.

Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats. Exp.Brain.Res. 235 3033 PMID:28725925 |Kim et al (2017) Characterising the mode of action of extracellular Connexin43 channel mimetic peptides in an in vitro ischemia injury model. Biochem.Biophys.Acta. 1861 68 PMID:27816754 |Tonkin et al (2017) Attenuation of mechanical pain hypersensitivity by treatment with Peptide5, a connexin-43 mimetic peptide, involves inhibition of NLRP3 inflammasome in nerve-injured mice. Exp.Neurol. 300 1 PMID:29055716

Gap 26 is a mimetic peptide corresponding to the residues 63-75 of connexin 43, which is a gap junction blocker.

BMT-090605 hydrochloride is an effective and selective inhibitor of connexin-2 associated kinase 1 (AAK1) (IC50=0.6 nM). BMT-090605 hydrochloride inhibits BMP-2 induced protein kinase (BIKE) (IC50=45 nM) and cyclin G-related kinase GAK (IC50=60 nM). BMT-090605 hydrochloride shows anti-injury activity. BMT-090605 hydrochloride has research value in neuropathic pain.

Gap 26 TFA, a gap junction blocker, is a connexin mimetic peptide derived from the amino acid sequence 63-75 in the first extracellular loop of connexin 43, featuring the SHVR amino acid motif [1].

Carbenoxolone (Biogastrone) is an inhibitor of 11β-HSD and gap junction connexin channels. Carbenoxolone inhibits macrophage migration into atria and prevents the development of fatty liver disease.

Peptide5 TFA, a connexin 43 mimetic peptide, mitigates swelling, astrogliosis, and neuronal cell death in animal models of spinal cord injury, and suppresses the NLRP3 inflammasome, functioning as an anti-inflammatory agent (1) (2) (3).

Zymosan A, a polysaccharide derived from Saccharomyces cerevisiae, is a TLR2 agonist that can upregulate ASCL2 through the TLR2 and Wnt signaling pathways, promoting the regeneration of intestinal stem cells (ISCs) after radiation-induced injury. It exhibits significant radioprotective effects, helping to prevent and alleviate IR-induced intestinal damage. Additionally, Zymosan A can induce immune responses, inflammation, anorexia, and elevated body temperature, and is commonly used to establish peritonitis models.

VRT-534 is a compound that selectively targets connexin 26 (Cx26), demonstrating dose-responsive binding to both wild-type (WT) Cx26 and the mutant Cx26 K188N, with EC50 values of 19 μM and 5 μM, respectively. It has potential applications in research concerning hearing impairment [1].

Carbenoxolone D4 is a deuterated compound of Carbenoxolone. Carbenoxolone (Biogastrone) is an inhibitor of 11β-HSD and gap junction connexin channels. Carbenoxolone inhibits macrophage migration into atria and prevents the development of fatty liver disease.

Gap 27 is a peptide(Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile) derived from connexin 43 that is a selective gap junction blocker.

Gap19 TFA is a peptide derived from nine amino acids of Cx43 cytoplasmic ring (CL), an effective, selective connexin 43 (Cx43) half-channel blocker.

TAPS sodium is a biological buffer that maintains the structural integrity of lysozyme and prevents thermal denaturation at elevated temperatures. With a pKa of 8.1, TAPS facilitates achieving half-maximal activity of the connexin protein channel.

(R,R)-VRT-534 is the (R,R)-enantiomer of VRT-534. VRT-534 (Compound 3) acts as a chemical chaperone targeting connexin 26 (Cx26). VRT-534 demonstrates dose-dependent binding with recombinant WT Cx26 and mutant Cx26 K188N, with EC50 values of 19 μM and 5 μM, respectively. VRT-534 is applicable in research related to hearing impairments.