Epsilon-V1-2 - ≥95% , CAS No.182683-50-7

CAS: 182683-50-7 Cat. No.: E651367 Molecular Weight: 843.96 PubChem CID: 10147482

GRADE & PURITY ≥95%

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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.

Form:Solid

IC50& Target:PKCε

Specifications

Specifications & Purity

≥95%

Biochemical and Physiological Mechanisms

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.

Storage

Desiccated, Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥95%

Names and Identifiers

• Canonical Smiles: CC(C)CC(C(=O)NC(CCCCN)C(=O)N1CCCC1C(=O)NC(C(C)O)C(=O)O)NC(=O)C(CO)NC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CCC(=O)O)N
• IUPAC Name: (4S)-4-amino-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[(2S)-2-[[(1S,2R)-1-carboxy-2-hydroxypropyl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
• InChIKey: KNTBAGOTDJPUJV-XMTFRXHISA-N
• INCHI: 1S/C37H65N9O13/c1-18(2)16-24(32(53)41-23(10-7-8-14-38)36(57)46-15-9-11-26(46)34(55)45-29(21(6)48)37(58)59)42-33(54)25(17-47)43-35(56)28(19(3)4)44-30(51)20(5)40-31(52)22(39)12-13-27(49)50/h18-26,28-29,47-48H,7-17,38-39H2,1-6H3,(H,40,52)(H,41,53)(H,42,54)(H,43,56)(H,44,51)(H,45,55)(H,49,50)(H,58,59)/t20-,21+,22-,23-,24-,25-,26-,28-,29-/m0/s1
• Isomeric SMILES: C[C@H]([C@@H](C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)N)O
• PubChem CID: 10147482
• Molecular Weight: 843.96

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organic acids and derivatives
    • Class Carboxylic acids and derivatives
      • Subclass Amino acids, peptides, and analogues
        • Level5 Peptides
          • Level6 Oligopeptides

• Kingdom: Organic compounds
• Superclass: Organic acids and derivatives
• Class: Carboxylic acids and derivatives
• Subclass: Amino acids, peptides, and analogues
• Intermediate Tree Nodes: Peptides
• Direct Parent: Oligopeptides
• Alternative Parents: Glutamic acid and derivatives Leucine and derivatives Valine and derivatives N-acyl-L-alpha-amino acids Proline and derivatives Serine and derivatives Alpha amino acid amides Alanine and derivatives Pyrrolidinecarboxamides N-acylpyrrolidines Short-chain hydroxy acids and derivatives Amino fatty acids Beta hydroxy acids and derivatives Branched fatty acids Heterocyclic fatty acids Hydroxy fatty acids Dicarboxylic acids and derivatives N-acyl amines Tertiary carboxylic acid amides Amino acids Secondary alcohols Secondary carboxylic acid amides Azacyclic compounds Carboxylic acids Hydrocarbon derivatives Carbonyl compounds Monoalkylamines Primary alcohols Organic oxides
• Molecular Framework: Aliphatic heteromonocyclic compounds
• Substituents: Alpha-oligopeptide - Glutamic acid or derivatives - Leucine or derivatives - Valine or derivatives - Proline or derivatives - N-acyl-l-alpha-amino acid - N-acyl-alpha-amino acid - N-acyl-alpha amino acid or derivatives - Alpha-amino acid amide - Serine or derivatives - Alanine or derivatives - N-substituted-alpha-amino acid - Alpha-amino acid or derivatives - Pyrrolidine-2-carboxamide - Pyrrolidine carboxylic acid or derivatives - N-acylpyrrolidine - Beta-hydroxy acid - Amino fatty acid - Short-chain hydroxy acid - Branched fatty acid - Heterocyclic fatty acid - Hydroxy fatty acid - Hydroxy acid - N-acyl-amine - Fatty acyl - Fatty acid - Fatty amide - Dicarboxylic acid or derivatives - Tertiary carboxylic acid amide - Pyrrolidine - Amino acid or derivatives - Amino acid - Carboxamide group - Secondary carboxylic acid amide - Secondary alcohol - Azacycle - Organoheterocyclic compound - Carboxylic acid - Organic nitrogen compound - Primary alcohol - Carbonyl group - Primary amine - Alcohol - Hydrocarbon derivative - Amine - Organic oxide - Organic oxygen compound - Organooxygen compound - Organonitrogen compound - Primary aliphatic amine - Aliphatic heteromonocyclic compound
• Description: This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Mechanisms of Action

Chemical and Physical Properties

• Solubility: H2O : 50 mg/mL (59.24 mM; Need ultrasonic)
• Molecular Weight: 844.000 g/mol
• XLogP3: -6.900
• Hydrogen Bond Donor Count: 12
• Hydrogen Bond Acceptor Count: 15
• Rotatable Bond Count: 26
• Exact Mass: 843.47 Da
• Monoisotopic Mass: 843.47 Da
• Topological Polar Surface Area: 362.000 Ų
• Heavy Atom Count: 59
• Formal Charge: 0
• Complexity: 1480.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 9
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 1