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 (385)
Related Products (385)
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Stearoyl-L-carnitine-d3
0 ImagesCat. No.: HY-113202SCAS No.: 1021439-31-5Stearoyl-L-carnitine-d3 is the deuterium labeled Stearoylcarnitine. Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2.
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BHA536
0 ImagesCat. No.: HY-164462CAS No.: 919992-85-1BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice.
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Mitoxantrone-d8 hydrochloride
0 ImagesCat. No.: HY-13502AS1Synonyms: Mitozantrone-d8 hydrochloride; NSC 301739-d8 hydrochlorideMitoxantrone-d8 (hydrochloride) (Mitozantrone-d8 (hydrochloride)) is deuterium labeled Mitoxantrone (dihydrochloride). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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PKCβII Peptide Inhibitor I
0 ImagesCat. No.: HY-P3199CAS No.: 862502-26-9PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction.
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Ruboxistaurin hydrochloride (Standard)
0 ImagesCat. No.: HY-10195BRCAS No.: 169939-93-9Synonyms: LY333531 hydrochloride (Standard)Ruboxistaurin hydrochloride (Standard) is the analytical standard of Ruboxistaurin hydrochloride (HY-10195B). This product is intended for research and analytical applications. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM.
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Daphnoretin (Standard)
0 ImagesDaphnoretin (Dephnoretin; Thymelol) (Standard) is the analytical standard of Daphnoretin (HY-N0699). This product is used for research and analytical applications. Daphnoretin is a protein kinase C (PKC) activator that can inhibit the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and has antiviral activity. Daphnoretin exerts its anti-tumor effect by inhibiting the activation of the PI3K/AKT signaling pathway, triggering the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and the activation of the NLRP3 inflammasome. Daphnoretin can regulate the differentiation and maturation of dendritic cells, by down-regulating the phosphorylation level of JNK, inhibiting its immune stimulating function, thereby playing a protective role in skin transplant rejection reactions.
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Mitoxantrone dihydrochloride (Standard)
0 ImagesSynonyms: Mitozantrone dihydrochloride (Standard); NSC 301739 dihydrochloride (Standard)Mitoxantrone (dihydrochloride) (Standard) is the analytical standard of Mitoxantrone (dihydrochloride). This product is intended for research and analytical applications. Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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R 59-022 (Standard)
0 ImagesSynonyms: DKGI-I (Standard); Diacylglycerol kinase inhibitor I (Standard)R 59-022 (Standard) is the analytical standard of R 59-022. This product is intended for research and analytical applications. R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
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Hispidin (Standard)
0 ImagesHispidin (Standard) is the analytical standard of Hispidin. This product is intended for research and analytical applications. Hispidin, a PKC inhibitor and a phenolic compound can be found in Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1][2][3][4][5][6][7].
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Protein kinase inhibitor H-7 (Standard)
0 ImagesCat. No.: HY-131900RCAS No.: 84477-87-2Protein kinase inhibitor H-7 (Standard) is the analytical standard of Protein kinase inhibitor H-7. This product is intended for research and analytical applications. Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC.
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Farnesylthiotriazole
0 ImagesCat. No.: HY-119818CAS No.: 156604-45-4Synonyms: FTT
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Ilmofosine
0 ImagesCat. No.: HY-133838CAS No.: 83519-04-4Synonyms: BM41440Ilmofosine (BM41440) is a potent and selective protein kinase C inhibitor. Ilmofosine induces cell cycle arrest at the G2 phase. Ilmofosine also is an anti-leishmanial agent.
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Ingenol Mebutate (Standard)
0 ImagesCat. No.: HY-B0719RCAS No.: 75567-37-2Synonyms: Ingenol 3-angelate (Standard); PEP005 (Standard)Ingenol Mebutate (Standard) is the analytical standard of Ingenol Mebutate. This product is intended for research and analytical applications. Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
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Protein kinase inhibitor H-7 dihydrochloride (Standard)
0 ImagesProtein kinase inhibitor H-7 (dihydrochloride) (Standard) is the analytical standard of Protein kinase inhibitor H-7 (dihydrochloride). This product is intended for research and analytical applications. Protein kinase inhibitor H-7 dihydrochloride is a potent PKC (protein kinase C) inhibitor. At 100 μM, Protein kinase inhibitor H-7 dihydrochloride completely inhibits both TPA (skin tumour promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase).
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1-Oleoyl-2-linoleoyl-sn-glycerol
0 ImagesCat. No.: HY-N15340CAS No.: 91125-76-7
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Desmethylglycitein (Standard)
0 ImagesCat. No.: HY-N5072RCAS No.: 17817-31-1Synonyms: 4',6,7-Trihydroxyisoflavone (Standard)Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
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K-252d
0 ImagesCat. No.: HY-130748CAS No.: 105114-22-5K-252d is an indolocarbazole alkaloid found in Nocardiopsis. It is a PKC inhibitor that inhibits PKC isolated from rat brain (IC50=350 nM). It also inhibits calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart (IC50=46.2 μM).
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Mitoxantrone (Standard)
0 ImagesSynonyms: Mitozantrone (Standard); NSC 301739 (Standard)Mitoxantrone (Standard) is the analytical standard of Mitoxantrone. This product is intended for research and analytical applications. Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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Ruboxistaurin (Standard)
0 ImagesCat. No.: HY-10195RCAS No.: 169939-94-0Synonyms: LY333531 (Standard)Ruboxistaurin (Standard) is the analytical standard of Ruboxistaurin. This product is intended for research and analytical applications. Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM.
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1,2-Dipentadecanoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodium
0 ImagesCat. No.: HY-W838254CAS No.: 322647-32-51,2-Dipentadecanoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodium functions as an activator for the protein kinase C family and is an anionic phospholipid found in mitochondrial and microsomal membranes, playing a crucial role in the composition of lung surfactant, particularly within the membranes of lamellar bodies in the lungs.
