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

PKC

Protein kinase C

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-119112A
    LY 379196
    Inhibitor
    LY 379196 is a PKC-β inhibitor (IC50: 50 nM and 30 nM for PKC βI and βII respectively). LY 379196 inhibits the VEGF, IGF-1 and bFGF-induced proliferation of bovine retinal microvascular endothelial cells (BREC). LY 379196 is an antiproliferatory agentfor proliferative retinopathy.
    LY 379196
  • HY-169578
    PKC-IN-5
    Inhibitor
    PKC-IN-5 (Compound PKCe2054) is a PKC inhibitor. PKC-IN-5 prevents the interaction between PKCe and its adaptor protein RACK2.
    PKC-IN-5
  • HY-N2344R
    Procyanidin A1 (Standard)
    Inhibitor
    Procyanidin A1 (Standard) is the analytical standard of Procyanidin A1. This product is intended for research and analytical applications. Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
    Procyanidin A1 (Standard)
  • HY-10341R
    Fasudil (Hydrochloride) (Standard)
    Inhibitor
    Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca2+ channel antagonist and vasodilator.
    Fasudil (Hydrochloride) (Standard)
  • HY-10343R
    Sotrastaurin (Standard)
    Inhibitor
    Sotrastaurin (Standard) is the analytical standard of Sotrastaurin. This product is intended for research and analytical applications. Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
    Sotrastaurin (Standard)
  • HY-117610
    Ro 31-8830
    Inhibitor
    Ro 31-8830 is an orally active, potent and selective inhibitor of protein kinase C with anti-inflammatory activity. Ro 31-8830 is promising for research of inflammatory disorders.
    Ro 31-8830
  • HY-141613A
    Dioleyl phosphatidylserine
    Activator
    Dioleyl phosphatidylserine is a phospholipid that can be used to form the cochlea. Dioleyl phosphatidylserine (100 μM) can activate PKC-γ under Ca2+ concentrations < 0.5 μM.
    Dioleyl phosphatidylserine
  • HY-167114
    (Rac)-Aurora A/PKC-IN-1
    Inhibitor
    (Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo.
    (Rac)-Aurora A/PKC-IN-1
  • HY-106381A
    Aurothiomalate tetramer sodium
    Inhibitor ≥98.0%
    Aurothiomalate tetramer sodium, an Aurothiomalate sodium (HY-106381) tetrameric form, is antiarthritic gold agent. Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor.
    Aurothiomalate tetramer sodium
  • HY-120463
    R8605
    Inhibitor
    R8605 is an inhibitor for PKC with an IC50 of 65 μM for PKC in rat brain. R8605 inhibits calcium/phospholipid-independent phosphorylation of protamine with IC50 of 70 μM and 100 μM. R8605 can be used in cancer research.
    R8605
  • HY-112384A
    Safingol hydrochloride
    Inhibitor
    Safingol hydrochloride is a lyso-sphingolipid PKC (protein kinase C ) inhibitor.
    Safingol hydrochloride
  • 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-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-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, VEGFR2/KDR/Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/Flt-1/2 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 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-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-100618R
    Hispidin (Standard)
    Inhibitor
    Hispidin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity

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