PKCε
PKCε is a novel protein kinase C isoform that functions as a serine/threonine signaling kinase and regulates proliferation, survival, motility, apoptosis, chemoresistance, and differentiation[1]. Mechanistically, PKCε connects receptor-driven DAG/phorbol ester-responsive signaling to oncogenic nodes including RhoA/C, STAT3, Akt, Rac1, EGFR-PLCγ, and p70S6K-linked insulin signaling[1][2][3]. In ischemia models, PKCε selectively translocates during ischemic preconditioning, and PKCε gene disruption abolishes infarct-size reduction in isolated mouse hearts[4][5]. In NSCLC models, PKCε supports Rac activation, membrane ruffling, migration, invasion, metastatic dissemination, and tumor growth[2][6]. Compared with related isoforms, PKCε shows a distinct profile: novel PKCs do not require calcium, PKCα and PKCδ can induce arrest in NSCLC cells, and PKCε instead drives G1-to-S progression and survival[1][2]. For experimental applications, εV1-2 pharmacologically inhibits PKCε-dependent Rac activation and motility, while εPKC activator peptides mimic ischemic preconditioning and contrast with δPKC inhibition in reperfusion injury studies[2][5].
Verweise:
- [1]. Gorin MA, et al. Protein kinase C epsilon: an oncogene and emerging tumor biomarker. Mol Cancer. 2009 Feb 19;8:9. [Content Brief]
- [2]. Caino MC, et al. Non-small cell lung carcinoma cell motility, rac activation and metastatic dissemination are mediated by protein kinase C epsilon. PLoS One. 2012;7(2):e31714. [Content Brief]
- [3]. Gassaway BM, et al. PKCε contributes to lipid-induced insulin resistance through cross talk with p70S6K and through previously unknown regulators of insulin signaling. Proc Natl Acad Sci U S A. 2018 Sep 18;115(38):E8996-E9005. [Content Brief]
- [4]. Ping P, et al. Ischemic preconditioning induces selective translocation of protein kinase C isoforms epsilon and eta in the heart of conscious rabbits without subcellular redistribution of total protein kinase C activity. Circ Res. 1997 Sep;81(3):404-14. [Content Brief]
- [5]. Inagaki K, et al. Additive protection of the ischemic heart ex vivo by combined treatment with delta-protein kinase C inhibitor and epsilon-protein kinase C activator. Circulation. 2003 Aug 19;108(7):869-75. [Content Brief]
- [6]. Caino MC, et al. Proteins kinase Cɛ is required for non-small cell lung carcinoma growth and regulates the expression of apoptotic genes. Oncogene. 2012 May 17;31(20):2593-600. [Content Brief]
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PKCε Verwandte Produkte (33)
Verwandte Produkte (33)
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Antibodies (1)
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Ruboxistaurin mesylate
0 ImagesSynonyms: LY333531 mesylateRuboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes.
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(S)-Ro 32-0432
0 ImagesArt. -Nr.: HY-108601ACAS. Nr.: 1781828-85-0(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
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Ro 31-8220
0 ImagesArt. -Nr.: HY-13866ACAS. Nr.: 125314-64-9Synonyms: Bisindolylmaleimide IXRo 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Ro 31-8220 can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.
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PKCiota-IN-2
0 ImagesArt. -Nr.: HY-122858CAS. Nr.: 2230055-52-2PKCiota-IN-2 (Compound 49) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
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PF-04577806
0 ImagesArt. -Nr.: HY-139467CAS. Nr.: 1072100-81-2
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AS2521780
0 ImagesArt. -Nr.: HY-12663CAS. Nr.: 1214726-89-2AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
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TAT-Epsilon-V1-2 TFA
0 ImagesArt. -Nr.: HY-P12125Reinheit: 99.89%TAT-Epsilon-V1-2 TFA is a cell-permeable PKCε peptide inhibitor. TAT-Epsilon-V1-2 TFA reduces chronic immune responses after heart transplantation. TAT-Epsilon-V1-2 TFA is applicable to research related to delayed graft function and acute kidney injury caused by renal ischemia-reperfusion injury.
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PKCiota-IN-1
0 ImagesArt. -Nr.: HY-122857CAS. Nr.: 2230052-97-6PKCiota-IN-1 (compound 51) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.7 nM. PKCiota-IN-1 also inhibits PKC-α and PKC-ε with IC50s of 45 nM and 450 nM, respectively.
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CIDD-0072424
0 ImagesArt. -Nr.: HY-158051CAS. Nr.: 1620195-03-0CIDD-0072424 selectively inhibits Protein Kinase C-epsilon (PKCε) (Ki=54 nM). CIDD-0072424 reduces ethanol consumption and preference in a dose-dependent manner.
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1,2-Dipalmitoyl-sn-glycerol (Standard)
0 ImagesArt. -Nr.: HY-W010736RCAS. Nr.: 30334-71-51,2-Dipalmitoyl-sn-glycerol (Standard) is the analytical standard of 1,2-Dipalmitoyl-sn-glycerol (HY-W010736). This product is intended for research and analytical applications. 1,2-Dipalmitoyl-sn-glycerol is a diacylglycerol that activates PKC. 1,2-Dipalmitoyl-sn-glycerol promotes GLUT4 translocation to the cell surface and recruitment to the plasma membrane of adipocytes. 1,2-Dipalmitoyl-sn-glycerol can be used in research on type 2 diabetes.
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Bisindolylmaleimide VIII
0 ImagesArt. -Nr.: HY-129624CAS. Nr.: 125313-65-7Synonyms: Ro 31-7549; Bis VIIIBisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
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Balanol
0 ImagesArt. -Nr.: HY-121197CAS. Nr.: 63590-19-2Synonyms: Ophiocordin; AzepinostatinBalanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides.
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