PKCε Inhibitor Peptide (Synonyms: Protein Kinase Cɛ Inhibitor Peptide，ɛV1-2) |
| رقم الكتالوجGC44655 |
PKCε ؛ المانع الببتيد (ε؛ -V1-2) ، PKCε ؛ الببتيد المشتق ، هو PKCε انتقائي ؛ المانع.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 182683-50-7
Sample solution is provided at 25 µL, 10mM.
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PKCε Inhibitor Peptide, also called εV1-2, is a protein kinase C ε (PKCε)-derived peptide, act as a selective PKCε inhibitor, inhibits the translocation of PKCε [1]. PKCε Inhibitor Peptide is a peptide designed to compete with native nPKC ε to bind ε-Receptors for activated C Kinase (ε-RACK) and thereby inhibits nPKC ε catalytic activity due to decreased substrate accessibility.
PKCε Inhibitor Peptide, a selective PKCε inhibitor, the addition of PKCε Inhibitor Peptide interferes with the interaction between PKCε and its anchoring protein, and abolishes the cardioprotective effects of PKCε [2]. ADP-induced thromboxane generation in human platelets pretreated with PKCε Inhibitor Peptide was more compared to the platelets pretreated with control peptide [4].
PKCε Inhibitor Peptide were used to inhibit PKCε expression and activity. Apigenin-7-O-β-D-(-6"-p-coumaroyl)-glucopyranoside (APG) preconditioning-induced PKCε translocation to the mitochondria and anti-mitochondrial oxidative stress effects were attenuated by PKCε-targeted ε-V1-2 treatment in IR-injured hearts [3].
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]. L. Tang, Y. Peng, T. Xu, X. Yi, Y. Liu, Y. Luo, D. Yin, M. He. The effects of quercetin protect cardiomyocytes from A/R injury is related to its capability to increasing expression and activity of PK C epsilon protein.Mol. Cell. Biochem., 382 (2013), pp. 145-152
[3]. Zhu Y, Di S, Hu W, et al.. A new flavonoid glycoside (APG) isolated from Clematis tangutica attenuates myocardial ischemia/reperfusion injury via activating PKCε signaling.Biochim Biophys Acta Mol Basis Dis. 2017; 1863:701-711. doi: 10.1016/j.bbadis.2016.12.013
[4]. Yamini Saraswathy Bynagari, B-Tech., Bela Nagy, M.D., et al. nPKC Epsilon Negatively Regulates Platelet Functional Responses 2008. Blood (2008) 112 (11): 2855.
| Cell experiment [1]: | |
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Cell lines |
Cardiomyocyte cells from 1- to 2-d-old Wistar rats |
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Preparation Method |
Cells incubated with a mixture of 100 µg/ml of Oleic acid (OA) and 400 µg/ml of bovine serum albumin for 12, 24, or 48 h at 37 °C, while the control group was treated with BSA alone for 24 or 48 h. To determine which protein kinases are activated by OA, the Src kinase inhibitor PP1 (10 µM) and three PKC inhibitors, calphostin C (a general PKC inhibitor; 500 nM), Gö6976 (a PKCa inhibitor; 1 µM), and peptide eV1–2 (a PKCe inhibitor; 1 µM), were used. The cells were incubated for 24 h with inhibitor alone or with OA plus inhibitor. |
|
Reaction Conditions |
1 µM for 24 hours |
|
Applications |
Calphostin C blocked OA-induced Cx43 Ser368 phosphorylation, showing involvement of PKC in this signaling cascade. In addition, PKCε Inhibitor Peptide, also blocked the effect, showing that PKCε was involved. |
| Animal experiment [2]: | |
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Animal models |
Male FVB (H-2q) and C57BL/6J (H-2b) mice |
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Preparation Method |
Recipient mice were treated with PKCε Inhibitor Peptide (n = 9, 20 mg/kg/day) or with TAT as a control (13 mg/kg/day; n = 8) using 0.1 mL osmotic pumps (release rate; 0.25 µL/h, 30 mM of each peptide in sterile saline) implanted subcutaneously on day 3, replaced on day 17 and left them until 30 days after transplantation. |
|
Dosage form |
osmotic pumps , 20 mg/kg/day |
|
Applications |
PKCε Inhibitor Peptide treatment significantly improved the beating score of cardiac allografts compared to TAT-peptide treatment, suggesting that adding PKCε Inhibitor Peptide treatment to CyA augmented preservation of graft function without toxic side effects. The beating score in the PKCε Inhibitor Peptide treated group at 30 days was equivalent to that after 14 days in the TAT control group |
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References: [1]: 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. |
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| Cas No. | 182683-50-7 | SDF | |
| المرادفات | Protein Kinase Cɛ Inhibitor Peptide，ɛV1-2 | ||
| Canonical SMILES | [H]N[C@@H](CCC(O)=O)C(N[C@H](C(N[C@@H](C(C)C)C(N[C@@H](CO)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N1CCC[C@H]1C(N[C@]([C@@H](C)O)([H])C(O)=O)=O)=O)=O)=O)=O)=O)C)=O | ||
| Formula | C37H65N9O13 | M.Wt | 844 |
| الذوبان | 100mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1848 mL | 5.9242 mL | 11.8483 mL |
| 5 mM | 0.237 mL | 1.1848 mL | 2.3697 mL |
| 10 mM | 0.1185 mL | 0.5924 mL | 1.1848 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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