PKC
Protein Kinase C Alpha (PKCα) is a serine/threonine kinase involved in diverse cellular processes including proliferation, differentiation, and apoptosis. It plays a critical role in signal transduction pathways downstream of G-protein-coupled receptors and receptor tyrosine kinases[1]. PKCα regulates cell survival and growth through activation of the MAPK/ERK and PI3K/AKT pathways[2]. In cancer, PKCα is often overexpressed and contributes to tumor progression, particularly in breast and prostate cancers[3]. It also modulates vascular smooth muscle contraction and endothelial function, implicating it in cardiovascular diseases. Notably, PKCα exhibits distinct functions compared to other PKC isoforms due to its unique subcellular localization and substrate specificity[4]. Targeting PKCα with selective inhibitors such as Gö6976 has shown therapeutic potential in preclinical models of cancer and inflammatory disorders[5].
References:
- [1]. Lee MJ, et al. Time to HIV rebound after infusion of long-acting broadly neutralising antibodies 3BNC117-LS and 10-1074-LS and analytical treatment interruption (the RIO trial): a double-blind, randomised, placebo-controlled trial. Lancet HIV. 2026 May 27:S2352-3018(26)00059-7. [Content Brief]
- [2]. Wolf S, et al. Selection for Evi1 activation in myelomonocytic leukemia induced by hyperactive signaling through wild-type NRas. Oncogene. 2013 Jun 20;32(25):3028-38. [Content Brief]
- [3]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]
- [4]. Kim JY, et al. The induction of STAT1 gene by activating transcription factor 3 contributes to pancreatic beta-cell apoptosis and its dysfunction in streptozotocin-treated mice. Cell Signal. 2010 Nov;22(11):1669-80. [Content Brief]
- [5]. Ciglenecki I, et al. Low sensitivity of the fourth-generation antigen/antibody HIV rapid diagnostic test Determine™ HIV Early Detect for detection of acute HIV infection at the point of care in rural Eswatini: a diagnostic accuracy study. J Int AIDS Soc. 2025 Jul;28(7):e26517. [Content Brief]
All Product Categories
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PKC Related Products (383)
Related Products (383)
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Punicic acid
0 ImagesPunicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways.
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Cercosporin
0 ImagesSynonyms: CGP049090Cercosporin is produced by a plant pathogen, Pseudocercosporella capsellae. Cercosporin is a potent photosensitizer with a short activation wavelength, mostly suitable for superficial photodynamic therapy (PDT) treatments, especially when it is necessary to avoid perforations. Cercosporin contains the perylenequinone structural features necessary to PKC activity with an IC50 of 0.6-1.3 μM.
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Ingenol 3,20-dibenzoate
0 ImagesIngenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells.
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Tigilanol tiglate
0 ImagesCat. No.: HY-109076CAS No.: 943001-56-7Synonyms: EBC-46Tigilanol tiglate (EBC-46) is a protein kinase C (PKC)/C1 domain activator. Tigilanol tiglate is associated with mitochondrial/endoplasmic reticulum (ER) dysfunction, leading to activation of the unfolded protein response (UPRmt/ER) and subsequent induction of ATP depletion, organelles expansion, Caspase activation, gasdermin E cleavage, and terminal necrosis. Tigilanol tiglate, as a small anti-tumor molecule with immunomodulatory effects, can be used in the study of head and neck squamous cell carcinoma and soft tissue sarcoma.
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Bisindolylmaleimide IV
0 ImagesSynonyms: Arcyriarubin ABisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
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Decursinol angelate
0 ImagesDecursinol angelate acts as a PKC activator and GDH inhibitor, with an IC50 of 1.432 μM against human GDH. Decursinol angelate activates PKC, downregulates PKCα and PKCβII isoforms, and exerts cytotoxic activity against cancer cells. Decursinol angelate binds to GDH and inhibits its enzymatic activity. Decursinol angelate inhibits VEGF-induced autophosphorylation of VEGFR2, downstream p42/44 ERK and JNK-MAPK signaling pathways, as well as the angiogenesis process. Decursinol angelate is applicable to research related to cancer and leukemia.
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Aprinocarsen sodium
0 ImagesSynonyms: ISIS 3521 sodiumAprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers.
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D-erythro-Sphingosine-d7
0 ImagesSynonyms: Erythrosphingosine-d7; erythro-C18-Sphingosine-d7; trans-4-Sphingenine-d7D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
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SBI-0087702
0 ImagesSBI-0087702 promots the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.
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C8-Ceramide
0 ImagesSynonyms: N-Octanoyl-D-erythro-sphingosineC8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
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SB 220025
0 ImagesSB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
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(rac)-AR-13503
0 ImagesSynonyms: (rac)-AR-13324 M1 metabolite(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice.
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Myelin basic protein (4-14) TFA
0 ImagesCat. No.: HY-P1821APurity: 99.41%Synonyms: MHP4-14 TFAMyelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts.
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Cholesterol sulfate-d7 sodium
0 ImagesCholesterol sulfate sodium-d7 is the deuterium labeled Cholesterol sulfate sodium. Cholesterol sulfate sodium is a naturally occurring, orally active cholesterol derivative that is widely distributed in various tissues and body fluids. Cholesterol sulfate sodium acts as a DOCK2 inhibitor, with IC50 values of 2 μM and 2.9 μM against mouse and human targets, respectively. Cholesterol sulfate sodium restricts excessive neutrophil infiltration and alleviates intestinal inflammation and damage. Cholesterol sulfate sodium serves as an activator of protein kinase C (PKC), which promotes squamous cell differentiation and inhibits skin carcinogenesis. Cholesterol sulfate sodium regulates cholesterol homeostasis and cellular metabolism by activating the AMPK-Sirt1 pathway. Cholesterol sulfate sodium can be used in research related to actinic keratitis, ulcerative colitis, skin cancer, and other conditions.
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DL-erythro-Dihydrosphingosine
0 ImagesDL-erythro-Dihydrosphingosine is a sphingosine-based PKC inhibitor. DL-erythro-Dihydrosphingosine directly inhibits the enzymatic activity of PLA2. DL-erythro-Dihydrosphingosine inhibits the activity of Bcl-2 protein involved in apoptosis. DL-erythro-Dihydrosphingosine inhibits the activity of matrix metalloproteinases (MMP). DL-erythro-Dihydrosphingosine is applicable for research on cancer and inflammatory diseases.
