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].
References:
- [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 Related Products (33)
Related Products (33)
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Antibodies (1)
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Midostaurin
0 ImagesSynonyms: PKC412; CGP 41251Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
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Rottlerin
0 ImagesRottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
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18:0-22:6 DG
0 ImagesSynonyms: 1-Stearoyl-2-docosahexaenoyl-sn-glycerol18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (Ki = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease.
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1,2-Dipalmitoyl-sn-glycerol-d9
0 ImagesCat. No.: HY-W010736SCAS No.: 1872379-48-01,2-Dipalmitoyl-sn-glycerol-d9 is the deuterated-labeled 1,2-Dipalmitoyl-sn-glycerol (HY-W010736). 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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KAI-1678
0 ImagesCat. No.: HY-P11803CAS No.: 1041004-14-1KAI-1678 is a selective protein kinase Cε (PKCε) inhibitor that competitively blocks the binding of PKCε to its anchoring protein RACK. KAI-1678 attenuates the responses of nociceptive neurons in rodent neuropathic pain models. KAI-1678 can be used in research related to moderate to severe postoperative pain, neuropathic pain, and postherpetic neuralgia.
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Ruboxistaurin
0 ImagesSynonyms: LY333531
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Ro 31-8220 mesylate
0 ImagesSynonyms: Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylateRo 31-8220 mesylate 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 mesylate 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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DCP-LA
0 ImagesSynonyms: FR236924DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis.
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(-)-Indolactam V
0 ImagesSynonyms: Indolactam V(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
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Epsilon-V1-2
0 ImagesCat. No.: HY-P0154CAS No.: 182683-50-7Synonyms: ε-V1-2; EAVSLKPT
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Ruboxistaurin hydrochloride
0 ImagesSynonyms: LY333531 hydrochloride
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Bisindolylmaleimide VIII acetate
0 ImagesSynonyms: Ro 31-7549 acetate; Bis VIII acetateBisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
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Ro 31-8220 formic
0 ImagesCat. No.: HY-13866BPurity: 99.76%Synonyms: Bisindolylmaleimide IX formicRo 31-8220 formic 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 formic also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively). Ro 31-8220 formic 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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1,2-Dipalmitoyl-sn-glycerol
0 Images1,2-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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PKCiota-IN-2 formic
0 ImagesCat. No.: HY-122858APurity: 99.04%PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 formic also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
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Bisindolylmaleimide XI hydrochloride
0 ImagesSynonyms: Ro 32-0432; Ro 31-8830 hydrochloride
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