PKCe Peptide Substrate

Product Name: PKCe Peptide Substrate

Sequence One Letter Code: ERMRPRKRQGSVRRRV

Sequence Three Letter Code: Glu-Arg-Met-Arg-Pro-Arg-Lys-Arg-Gln-Gly-Ser-Val-Arg-Arg-Arg-Val

Cas No: 120253-69-2

Chemical Formula:C83H155N39O21S

Molecular Weight: 2067.5

Purity: 95%

Form: Lyophilized

Storage Conditions: - 20 °C

Research Area: peptide substrate

SMILES: CC(C)C(C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(C(C)C)C(=O)O)NC(=O)C(CO)NC(=O)CNC(=O)C(CCC(=O)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCCN)NC(=O)C(CCCNC(=N)N)NC(=O)C1CCCN1C(=O)C(CCCNC(=N)N)NC(=O)C(CCSC)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCC(=O)O)N

IUPAC: 4-amino-5-[[1-[[1-[[1-[2-[[1-[[6-amino-1-[[1-[[5-amino-1-[[2-[[1-[[1-[[5-carbamimidamido-1-[[5-carbamimidamido-1-[[5-carbamimidamido-1-[(1-carboxy-2-methylpropyl)amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid

INCHIKEY: RLQBYTJEMHGNOD-UHFFFAOYSA-N

INCHI:

InChI=1S/C83H155N39O21S/c1-42(2)60(74(140)118-50(21-12-35-105-81(95)96)69(135)113-47(18-9-32-102-78(89)90)66(132)114-51(22-13-36-106-82(97)98)71(137)121-61(43(3)4)76(142)143)120-72(138)55(41-123)109-58(125)40-108-63(129)52(26-27-57(86)124)115-67(133)48(19-10-33-103-79(91)92)112-64(130)45(16-6-7-30-84)111-68(134)49(20-11-34-104-80(93)94)117-73(139)56-24-15-38-122(56)75(141)54(23-14-37-107-83(99)100)119-70(136)53(29-39-144-5)116-65(131)46(17-8-31-101-77(87)88)110-62(128)44(85)25-28-59(126)127/h42-56,60-61,123H,6-41,84-85H2,1-5H3,(H2,86,124)(H,108,129)(H,109,125)(H,110,128)(H,111,134)(H,112,130)(H,113,135)(H,114,132)(H,115,133)(H,116,131)(H,117,139)(H,118,140)(H,119,136)(H,120,138)(H,121,137)(H,126,127)(H,142,143)(H4,87,88,101)(H4,89,90,102)(H4,91,92,103)(H4,93,94,104)(H4,95,96,105)(H4,97,98,106)(H4,99,100,107)

Source / Species: Zebrafish, Xenopus

Conjugation: Unconjugated

Code Nacres: NA.26

Application: PKCε Peptide Substrate is a synthetic peptide derived from the pseudosubstrate region of the epsilon isoform of protein kinase C, modified by substitution of alanine with serine to create a phosphorylatable sequence. This alteration enables selective recognition and phosphorylation by PKCε, which exhibits apparent substrate specificity with a Km of approximately 68 µM. PKCε plays important roles in regulating cell proliferation, survival, differentiation, and stress responses across multiple tissues. The peptide substrate is widely used in in vitro kinase assays to quantify PKCε catalytic activity and determine kinetic parameters. It also supports screening and characterization of isoform-selective modulators targeting PKC signaling pathways. By enabling precise measurement of PKCε-dependent phosphorylation, this substrate facilitates mechanistic studies of isoform-specific signaling and contributes to therapeutic research focused on PKC-regulated cellular processes.

Current Research: PKCε Peptide Substrate is a synthetic peptide derived from the pseudosubstrate region of the epsilon isoform of protein kinase C (PKCε). In its native form, the pseudosubstrate domain contains an alanine residue at the position corresponding to the phosphorylation site, preventing autophosphorylation and maintaining the kinase in an inactive conformation. In this engineered substrate, alanine is replaced with serine, creating a phosphorylatable sequence that enables selective catalytic turnover by PKCε in vitro. This rational modification converts a regulatory motif into a functional assay substrate while preserving isoform-relevant sequence context. PKCε belongs to the novel PKC (nPKC) subfamily, which is activated by diacylglycerol and phospholipids but is calcium independent. It is widely expressed and plays critical roles in cell proliferation, survival signaling, differentiation, cytoskeletal organization, and stress adaptation. Dysregulation of PKCε activity has been implicated in oncogenesis, cardioprotection mechanisms, metabolic regulation, and inflammatory responses. Because individual PKC isoforms often exert distinct and sometimes opposing biological effects, isoform-specific activity assessment is essential for mechanistic clarity. The PKCε Peptide Substrate supports direct quantification of kinase activity in biochemical assays. With an apparent Km of approximately 68 µM, the peptide demonstrates efficient recognition and phosphorylation by PKCε under optimized conditions. In vitro kinase assays using this substrate allow measurement of phosphate incorporation via radiometric detection, phospho-specific antibody recognition, or fluorescence- and luminescence-coupled methods. These formats enable both endpoint and kinetic analysis of catalytic turnover. A key application of this substrate is determination of kinetic parameters, including Km and Vmax, to characterize enzyme efficiency and substrate affinity. Such measurements are particularly useful when comparing wild-type PKCε with mutant variants or evaluating regulatory effects of cofactors such as diacylglycerol analogs and phospholipids. By providing a defined and reproducible phosphorylation site, the peptide minimizes variability associated with complex protein substrates. The substrate is also well suited for screening and characterization of PKC modulators. Development of isoform-selective inhibitors remains an important objective in therapeutic research, given the broad involvement of PKC signaling in cancer, cardiovascular disease, and metabolic disorders. Using a PKCε-specific peptide substrate allows researchers to evaluate compound potency and selectivity directly at the catalytic level, supporting structure–activity relationship studies and optimization of targeted inhibitors. Beyond drug discovery, the peptide facilitates mechanistic studies of PKCε-dependent signaling pathways. By integrating substrate phosphorylation assays with downstream readouts—such as ERK activation, NF-κB signaling, or cytoskeletal reorganization—investigators can correlate enzymatic activity with functional cellular outcomes. This approach enhances understanding of how PKCε regulates context-dependent signaling networks. In summary, PKCε Peptide Substrate provides a targeted and reliable platform for measuring isoform-specific kinase activity. Its rationally engineered phosphorylation site, compatibility with diverse detection methods, and suitability for kinetic and inhibitor studies make it a valuable reagent for dissecting PKCε-mediated signaling. Through precise quantification of PKCε-dependent phosphorylation, this substrate supports both fundamental research and therapeutic development focused on PKC-regulated cellular processes.