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-117800
    BJE6-106
    		Inhibitor 99.93%
    BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
    BJE6-106
  • HY-10195
    Ruboxistaurin
    		Inhibitor 99.90%
    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.
    Ruboxistaurin
  • HY-103045
    CMPD101
    		Inhibitor 98.95%
    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
  • HY-107421
    Prostratin
    		Activator 99.80%
    Prostratin, a natural terpenoid compound, is a PKC activator, with a Ki of 12.5 nM and shows inhibitory effect on HIV-1.
    Prostratin
  • HY-107613
    R 59-022
    		Activator 99.82%
    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
  • HY-12307
    (-)-Indolactam V
    		Activator 98.75%
    (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
    (-)-Indolactam V
  • HY-N0865
    Ingenol
    		Activator 99.51%
    Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
    Ingenol
  • HY-13772
    Valrubicin
    		Inhibitor 99.60%
    Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
    Valrubicin
  • HY-132304
    CC-90005
    		Inhibitor 99.67%
    CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by inhibiting IL-2 expression.
    CC-90005
  • HY-131648
    1-Oleoyl-2-acetyl-sn-glycerol
    		Activator 99.90%
    1-Oleoyl-2-acetyl-sn glycerol is a synthetic, cell permeable diacylglycerol analog. 1-Oleoyl-2-acetyl-sn glycerol activates calcium-dependent protein kinase C (PKC) and induces the superoxide-production.
    1-Oleoyl-2-acetyl-sn-glycerol
  • HY-126146
    PKC-iota inhibitor 1
    		Inhibitor 99.76%
    PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ℩) inhibitor with an IC50 value of 0.34 μM.
    PKC-iota inhibitor 1
  • HY-P0154
    Epsilon-V1-2
    		Inhibitor
    Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
    Epsilon-V1-2
  • HY-118384
    Sangivamycin
    		Inhibitor
    Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.
    Sangivamycin
  • HY-100618
    Hispidin
    		Inhibitor 99.94%
    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.
    Hispidin
  • HY-112782
    VTX-27
    		Inhibitor 99.02%
    VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
    VTX-27
  • HY-N0152
    Myricitrin
    		Inhibitor 99.64%
    Myricitrin, a naturally occurring flavonoid, is an orally active nitric oxide (NO) and PKC inhibitor. Myricitrin has central nervous system activity, including anxiolytic-like action. Myricitrin possesses antioxidant, anti-inflammatory, antifibrotic and anti-malarial effects.
    Myricitrin
  • HY-13335
    PKCβ inhibitor 1
    		Inhibitor 99.40%
    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
    PKCβ inhibitor 1
  • HY-16903
    PKC-IN-1
    		Inhibitor 99.79%
    PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
    PKC-IN-1
  • HY-112681
    PKC-theta inhibitor 2
    		Inhibitor 99.37%
    PKC-theta inhibitor 2 is a potent and selective PKC-θ inhibitor with an IC50 value of 18 nM.
    PKC-theta inhibitor 2
  • HY-106262B
    Delcasertib hydrochloride
    		Inhibitor 99.86%
    Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
    Delcasertib hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
PKC Isoform Comparison

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