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
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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J mice transplanted the hearts of FVB miceDosage: 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.
