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-116060
    RK-286D
    Inhibitor
    RK-286D is an antibiotic and a PKC inhibitor with antimicrobial activity. RK-286D shows inhibitory activities against bleb formation induced by PDBu (HY-18985) and in vitro PKC activity.
    RK-286D
  • HY-113202S1
    Stearoyl-L-carnitine-d9 chloride
    Inhibitor
    Stearoyl-L-carnitine-d9 chloride is the deuterium labeled Stearoyl-L-carnitine chloride. Stearoyl-L-carnitine chloride, a fatty ester lipid molecule, is an endogenous metabolite. Stearoyl-L-carnitine chloride can be used as PKC inhibitor. Stearoyl-L-carnitine chloride accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoyl-L-carnitine chloride inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoyl-L-carnitine chloride acts as a metabolomics biomarker for Parkinson’s disease. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2.
    Stearoyl-L-carnitine-d<sub>9</sub> chloride
  • HY-10341D
    Fasudil mesylate
    Inhibitor
    Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active 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 mesylate is also a potent Ca2+ channel antagonist and vasodilator.
    Fasudil mesylate
  • 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-13866R
    Ro 31-8220 mesylate (Standard)
    Inhibitor
    Ro 31-8220 mesylate (Standard) is the analytical standard of Ro 31-8220 mesylate (HY-13866). This product is intended for research and analytical applications. Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Ro 31-8220 mesylate can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.
    Ro 31-8220 mesylate (Standard)
  • 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-13867AR
    Bisindolylmaleimide I hydrochloride (Standard)
    Inhibitor
    Bisindolylmaleimide I (hydrochloride) (Standard) is the analytical standard of Bisindolylmaleimide I (hydrochloride). This product is intended for research and analytical applications. Bisindolylmaleimide I (GF109203X) hydrochloride 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 hydrochloride is also a GSK-3 inhibitor.
    Bisindolylmaleimide I hydrochloride (Standard)
  • HY-N2110R
    Phellopterin (Standard)
    Inhibitor
    Phellopterin (Standard) is the analytical standard of Phellopterin. Phellopterin, 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.
    Phellopterin (Standard)
  • HY-18739R
    Phorbol 12-myristate 13-acetate (Standard)
    Activator
    Phorbol 12-myristate 13-acetate (Standard) is the analytical standard of Phorbol 12-myristate 13-acetate. This product is intended for research and analytical applications. Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells (Validated by MedChemExpress (MCE)).
    Phorbol 12-myristate 13-acetate (Standard)
  • 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-N2180R
    Pinoresinol dimethyl ether (Standard)
    Activator
    Pinoresinol dimethyl ether (Standard) is the analytical standard of Pinoresinol dimethyl ether (HY-N2180). This product is intended for research and analytical applications. Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furanoid lignin. Pinoresinol dimethyl ether can be isolated from Magnolia biondii. Pinoresinol dimethyl ether activates MAPK, PKC, and PKA upstream pathways and inhibits NO levels. Pinoresinol dimethyl ether has neuroprotective activity.
    Pinoresinol dimethyl ether (Standard)
  • HY-18965R
    TAS-301 (Standard)
    Inhibitor
    TAS-301 (Standard) is the analytical standard of TAS-301. This product is intended for research and analytical applications. TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
    TAS-301 (Standard)
  • HY-112384A
    Safingol hydrochloride
    Inhibitor
    Safingol hydrochloride is a lyso-sphingolipid PKC (protein kinase C ) inhibitor.
    Safingol hydrochloride
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