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

PKC

Protein kinase C

PKC

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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-122241
    MT477
    		Inhibitor
    MT477 is a potent protein kinase C (PKC) inhibitor. MT477 induces apoptosis and necrosis. MT477 decreases the protein expression of Ras-GTP, p-Erk1/2, p-Elk1. MT477 shows antitumor activity.
    MT477
  • HY-108600R
    CGP-53353 (Standard)
    		Inhibitor
    CGP-53353 (Standard) is the analytical standard of CGP-53353 (HY-108600). This product is intended for research and analytical applications. CGP-53353 (DAPH-7) is an potent PKC inhibitor with IC50s of 0.41 μM and 3.8 μM for PKCβII and PKCβI, respectively. CGP-53353 can inhibit glucose-induced cell proliferation and DNA synthesis in AoSMC and A10 cells. CGP-53353 can be used for researching atherosclerosis of diabetic patients.
    CGP-53353 (Standard)
  • HY-108254R
    Bisindolylmaleimide IV (Standard)
    		Inhibitor
    Bisindolylmaleimide IV (Standard) is the analytical standard of Bisindolylmaleimide IV. This product is intended for research and analytical applications. Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
    Bisindolylmaleimide IV (Standard)
  • 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-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-103045R
    CMPD101 (Standard)
    		Inhibitor
    CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
    CMPD101 (Standard)
  • 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-183530
    p38 MAPK-IN-11
    		Inhibitor
    p38 MAPK-IN-11 is a CSBP (p38 MAPK) kinase inhibitor with IC50 values of 0.15 μM (binding activity) and 0.21 μM (inhibitory activity). p38 MAPK-IN-11 shows weak inhibitory activity against PKCα kinase, with an IC50 of 7.6 μM. p38 MAPK-IN-11 inhibits the production of IL-1. p38 MAPK-IN-11 also acts as a β-lactam antibiotic potentiator, but has no antibacterial activity itself.
    p38 MAPK-IN-11
  • 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-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
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
PKC Isoform Comparison

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