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182683-50-7

182683-50-7 structure
182683-50-7 structure
  • Name: Epsilon-V1-2
  • Chemical Name: PKCε Inhibitor Peptide
  • CAS Number: 182683-50-7
  • Molecular Formula: C37H65N9O13
  • Molecular Weight: 843.964
  • Catalog: Signaling Pathways Epigenetics PKC
  • Create Date: 2021-05-10 23:22:30
  • Modify Date: 2024-01-02 00:52:08
  • Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC[1].

Name PKCε Inhibitor Peptide
Synonyms L-Threonine, L-α-glutamyl-L-alanyl-L-valyl-L-seryl-L-leucyl-L-lysyl-L-prolyl-
L-α-Glutamyl-L-alanyl-L-valyl-L-seryl-L-leucyl-L-lysyl-L-prolyl-L-threonine
PKCε Inhibitor Peptide
Description Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC[1].
Related Catalog
Target

PKCε

In Vitro Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide containing the site for its specific receptor for activated C kinase (RACK), inhibits translocation of PKCε and reduces insulin response to glucose[1]. Epsilon-V1-2 (ε-V1-2; 1 µM, 24 hours) treatment significantly inhibits Oleic acid (OA)-induced connexin 43 (Cx43) Ser368 phosphorylation and prevents OA-induced gap junction disassembly in cardiomyocytes[2].
In Vivo Epsilon-V1-2 (20 mg/kg/day; osmotic pumps; daily; for 4 weeks) treatment significantly improves the beating score in a murine heterotopic transplantation model. Epsilon-V1-2 reduces infiltration of macrophages and T cells into the cardiac grafts, and decreases parenchymal fibrosis. Epsilon-V1-2 treatment almost abolishes the rise in pro-fibrotic cytokine, TGF-β and monocyte recruiting chemokine MCP-1 levels[3]. Animal Model: C57BL/6J mice transplanted the hearts of FVB mice[3] Dosage: 20 mg/kg/day Administration: 0.1 mL osmotic pumps implanted subcutaneously; daily; for 4 weeks Result: Significantly improved the beating score throughout the treatment.
References

[1]. M Yedovitzky, et al. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J Biol Chem. 1997 Jan 17;272(3):1417-20.

[2]. Yuahn-Sieh Huang, et al. Mechanism of oleic acid-induced gap junctional disassembly in rat cardiomyocytes. J Mol Cell Cardiol. 2004 Sep;37(3):755-66.

[3]. Tomoyoshi Koyanagi, et al. Pharmacological inhibition of epsilon PKC suppresses chronic inflammation in murine cardiac transplantation model. J Mol Cell Cardiol. 2007 Oct;43(4):517-22.

Density 1.3±0.1 g/cm3
Boiling Point 1280.1±65.0 °C at 760 mmHg
Molecular Formula C37H65N9O13
Molecular Weight 843.964
Flash Point 728.0±34.3 °C
Exact Mass 843.470154
LogP -1.22
Vapour Pressure 0.0±0.6 mmHg at 25°C
Index of Refraction 1.552