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 (384)
Related Products (384)
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Sangivamycin
0 ImagesCat. No.: HY-118384CAS No.: 18417-89-5Synonyms: NSC 65346; BA-90912Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.
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ZIP
0 ImagesZIP is a selective peptide inhibitor of PKMζ. ZIP injections can block the impairment in morphine conditioned place preference induced.
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AR-13503
0 ImagesSynonyms: AR-13324 M1 metaboliteAR-13503 (AR-13324 M1 metabolite) is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research.
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Myelin Basic Protein
0 ImagesSynonyms: MHP4-14Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein 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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Phellopterin
0 ImagesPhellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.
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MANS peptide TFA
0 ImagesCat. No.: HY-P10218APurity: 99.32%MANS peptide TFA is the TFA salt form of MANS peptide (HY-P10218). MANS peptide TFA is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis.
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p32 Inhibitor M36
0 ImagesSynonyms: M36p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
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Bisindolylmaleimide I hydrochloride
0 ImagesSynonyms: GF109203X hydrochloride; Go 6850 hydrochloride
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Bisindolylmaleimide X hydrochloride
0 ImagesSynonyms: BIM-X hydrochloride; Ro31-8425 hydrochlorideBisindolylmaleimide X hydrochloride(Ro 31-8425 hydrochloride, BIM-X hydrochloride) is a cell-penetrating PKC inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM. Bisindolylmaleimide X hydrochloride inhibits the proliferation of CD4 T cells in vitro. Bisindolylmaleimide X hydrochloride inhibits eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. Bisindolylmaleimide X hydrochloride can be used for research on the immune system and cardiovascular diseases.
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1-Stearoyl-2-arachidonoyl-sn-glycerol
0 Images1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity.
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Phorbol 12-myristate 13-acetate (Standard)
0 ImagesCat. No.: HY-18739RCAS No.: 16561-29-8Synonyms: PMA (Standard); TPA (Standard); Phorbol myristate acetate (Standard)Phorbol 12-myristate 13-acetate (PMA; TPA; Phorbol myristate acetate) (Standard) is the analytical standard of Phorbol 12-myristate 13-acetate. This product is intended for research and analytical applications.
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(+)-Eudesmin
0 ImagesSynonyms: (+)-Eudesmine
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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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N-Desmethyltamoxifen hydrochloride
0 ImagesN-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
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Forskolin (Standard)
0 ImagesSynonyms: Coleonol (Standard); Colforsin (Standard); HL 362 (Standard)Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
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MPSD TFA
0 ImagesCat. No.: HY-P10471APurity: 99.38%Synonyms: MARCKS-ED TFAMPSD TFA (MARCKS-ED TFA) is the TFA salt form of MPSD (HY-P10471). MPSD TFA is a 25-amino acid peptide based on the effector domain sequence of the intracellular membrane protein myristoylated alanine-rich C-kinase substrate (MARCKS). MPSD TFA can sense membrane curvature and recognize phosphatidylserine. MPSD TFA can be utilized as biological probe to study membrane shape and lipid composition.
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Calphostin C
0 ImagesSynonyms: UCN-1028CCalphostin C is a highly selective PKC inhibitor (IC50=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications.
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Protein kinase inhibitor H-7
0 ImagesProtein kinase inhibitor H-7 is a selective inhibitor of PKC and cyclic nucleotide-dependent protein kinases, with a Ki value of 6.0 μM for rabbit protein kinase C, a Ki value of 3.0 μM for rabbit cAMP-dependent protein kinase, and a Ki value of 5.8 μM for porcine cGMP-dependent protein kinase. Protein kinase inhibitor H-7 has no effect on Ca2+-calmodulin-dependent enzymes. Protein kinase inhibitor H-7 regulates the Actin cytoskeleton, inhibits contractility, disrupts stress fibers, induces protrusive activity, stabilizes intercellular junctions, and triggers rapid and reversible cytoskeletal reorganization. Protein kinase inhibitor H-7 serves as a research tool for elucidating the functions of protein kinase C-mediated signaling systems.
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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.
