2. Signaling Pathways
  3. Epigenetics
    TGF-beta/Smad
  4. PKC

PKC

Protein kinase C

PKC

Related Products

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PKC (Protein kinase C) is a family of protein kinase enzymes that are involved in controlling the function of otherproteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins. PKC enzymes in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca2+). Hence PKC enzymes play important roles in several signal transduction cascades. The PKC family consists of 15 isozymes in humans: PKC-α (PRKCA), PKC-β1 (PRKCB), PKC-β2 (PRKCB), PKC-γ (PRKCG), PKC-δ (PRKCD), PKC-δ1 (PRKD1), PKC-δ2 (PRKD2), PKC-δ3 (PRKD3), PKC-ε (PRKCE), PKC-η (PRKCH), PKC-θ (PRKCQ), PKC-ι (PRKCI), PKC-ζ (PRKCZ), PK-N1 (PKN1), PK-N2 (PKN2), PK-N3 (PKN3). PKC is involved in receptor desensitization, in modulating membrane structure events, in regulating transcription, in mediating immune responses, in regulating cell growth, and in learning and memory. These functions are achieved by PKC-mediated phosphorylation of other proteins.

PKC Isoform Specific Products:

PKC Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-129624
    Bisindolylmaleimide VIII
    		Inhibitor
    Bisindolylmaleimide 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.
    Bisindolylmaleimide VIII
  • HY-13867R
    Bisindolylmaleimide I (Standard)
    		Inhibitor
    Bisindolylmaleimide I (Standard) is the analytical standard of Bisindolylmaleimide I. This product is intended for research and analytical applications. Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor.
    Bisindolylmaleimide I (Standard)
  • HY-13661
    7-Hydroxystaurosporine
    		Inhibitor
    7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis.
    7-Hydroxystaurosporine
  • HY-W114420
    3-Methyl-L-tyrosine
    3-Methyl-L-tyrosine is a derivative of L-Tyrosine (HY-N0473). Structurally, 3-Methyl-L-tyrosine features a methyl modification at the third position of the aromatic ring of L-Tyrosine. As a substrate for the protein tyrosine kinase Csk, 3-Methyl-L-tyrosine's relative catalytic efficiency (kcat/Km) is 38% of L-Tyrosine, indicating that the methyl modification impacts the processing efficiency of Gsk significantly. 3-Methyl-L-tyrosine helps to deepen the understanding of Gsk's molecular recognition mechanisms of its substrates, which is crucial for developing specific inhibitors targeting Gsk.
    3-Methyl-L-tyrosine
  • HY-113202S
    Stearoyl-L-carnitine-d3
    		Inhibitor
    Stearoyl-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.
    Stearoyl-L-carnitine-d<sub>3</sub>
  • HY-10230R
    Midostaurin (Standard)
    		Inhibitor
    Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (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.
    Midostaurin (Standard)
  • HY-164462
    BHA536
    		Inhibitor
    BHA536 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.
    BHA536
  • HY-13502AS1
    Mitoxantrone-d8 hydrochloride
    		Inhibitor
    Mitoxantrone-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.
    Mitoxantrone-d<sub>8</sub> hydrochloride
  • HY-P3199
    PKCβII Peptide Inhibitor I
    		Inhibitor
    PKCβII 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.
    PKCβII Peptide Inhibitor I
  • HY-N0699R
    Daphnoretin (Standard)
    		Activator
    Daphnoretin (Standard) is the analytical standard of Daphnoretin. This product is intended for research and analytical applications. Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst.
    Daphnoretin (Standard)
  • HY-13502AR
    Mitoxantrone dihydrochloride (Standard)
    		Inhibitor
    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.
    Mitoxantrone dihydrochloride (Standard)
  • HY-107613R
    R 59-022 (Standard)
    		Activator
    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.
    R 59-022 (Standard)
  • HY-100618R
    Hispidin (Standard)
    		Inhibitor
    Hispidin (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].
    Hispidin (Standard)
  • HY-121197
    Balanol
    		Inhibitor
    Balanol (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.
    Balanol
  • HY-131900R
    Protein kinase inhibitor H-7 (Standard)
    		Inhibitor
    Protein 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.
    Protein kinase inhibitor H-7 (Standard)
  • HY-119818
    Farnesylthiotriazole
    		Activator
    Farnesylthiotriazole (FTT) is a PKC activator (Kd=0.8 μM) that can be used in cancer research.
    Farnesylthiotriazole
  • HY-133838
    Ilmofosine
    		Inhibitor
    Ilmofosine (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.
    Ilmofosine
  • HY-B0719R
    Ingenol Mebutate (Standard)
    		Modulator
    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.
    Ingenol Mebutate (Standard)
  • HY-B0340R
    Nefiracetam (Standard)
    		Activator
    Nefiracetam (Standard) is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
    Nefiracetam (Standard)
  • HY-100983R
    Protein kinase inhibitor H-7 dihydrochloride (Standard)
    		Inhibitor
    Protein 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).
    Protein kinase inhibitor H-7 dihydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
PKC Isoform Comparison

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