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-108391
    C8-Ceramide
    		Activator 98.0%
    C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
    C8-Ceramide
  • HY-14604
    Xaliproden hydrochloride
    		Activator 98.40%
    Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.
    Xaliproden hydrochloride
  • HY-125639
    (rac)-AR-13503
    		Inhibitor 99.08%
    (rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice.
    (rac)-AR-13503
  • HY-18719A
    Endoxifen Z-isomer hydrochloride
    		Inhibitor 99.67%
    Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer hydrochloride inhibits PKCβ1 kinase activity. Endoxifen Z-isomer hydrochloride attenuates PKCβ1-activated AKTSer473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer hydrochloride exhibits anticancer activity against hormone-resistant metastatic breast cancer.
    Endoxifen Z-isomer hydrochloride
  • HY-108604
    Bisindolylmaleimide II
    		Inhibitor 99.96%
    Bisindolylmaleimide II is a general inhibitor of all PKC subtypes.
    Bisindolylmaleimide II
  • HY-P1821A
    Myelin basic protein (4-14) TFA
    		99.41%
    Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts.
    Myelin basic protein (4-14) TFA
  • HY-112291
    SB 220025
    		Inhibitor 99.90%
    SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
    SB 220025
  • HY-134963
    SBI-0087702
    		99.55%
    SBI-0087702 promots the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.
    SBI-0087702
  • HY-P10218
    MANS peptide
    		Inhibitor 99.66%
    MANS peptide is an inhibitor for myristoylated alanine-rich C kinase substrate (MARCKS), which competes with MARCKS in cells for membrane binding, and thus inhibits the stimulation of mucin secretion and tumor metastasis.
    MANS peptide
  • HY-111355S
    Cholesterol sulfate-d7 sodium
    		Inhibitor 99.70%
    Cholesterol sulfate sodium-d7 is the deuterium labeled Cholesterol sulfate sodium. Cholesterol sulfate sodium is a naturally occurring, orally active cholesterol derivative that is widely distributed in various tissues and body fluids. Cholesterol sulfate sodium acts as a DOCK2 inhibitor, with IC50 values of 2 μM and 2.9 μM against mouse and human targets, respectively. Cholesterol sulfate sodium restricts excessive neutrophil infiltration and alleviates intestinal inflammation and damage. Cholesterol sulfate sodium serves as an activator of protein kinase C (PKC), which promotes squamous cell differentiation and inhibits skin carcinogenesis. Cholesterol sulfate sodium regulates cholesterol homeostasis and cellular metabolism by activating the AMPK-Sirt1 pathway. Cholesterol sulfate sodium can be used in research related to actinic keratitis, ulcerative colitis, skin cancer, and other conditions.
    Cholesterol sulfate-d<sub>7</sub> sodium
  • HY-W013852
    PKC-IN-6
    		Inhibitor 99.93%
    PKC-IN-6 is a selective inhibitor of protein kinase C-α (PKC-α) with an IC50 of 240 μM. PKC-IN-6 shows no inhibitory activity against PKC-δ, PKA or EGF-R tyrosine kinase. PKC-IN-6 can be used in research related to bladder cancer.
    PKC-IN-6
  • HY-101195
    DL-erythro-Dihydrosphingosine
    		Inhibitor 98.0%
    DL-erythro-Dihydrosphingosine is a sphingosine-based PKC inhibitor. DL-erythro-Dihydrosphingosine directly inhibits the enzymatic activity of PLA2. DL-erythro-Dihydrosphingosine inhibits the activity of Bcl-2 protein involved in apoptosis. DL-erythro-Dihydrosphingosine inhibits the activity of matrix metalloproteinases (MMP). DL-erythro-Dihydrosphingosine is applicable for research on cancer and inflammatory diseases.
    DL-erythro-Dihydrosphingosine
  • HY-P10532
    Myelin basic protein, MBP (68-86)
    		99.86%
    Myelin basic protein, MBP (68-86) is the portion of the 68th to 86th amino acid residues in the MBP protein sequence. Myelin basic protein, MBP (68-86) can act as an autoantigen, triggering the immune system to attack its own myelin. Myelin basic protein, MBP (68-86) is used as one of the immunogens in the experimental autoimmune encephalomyelitis (EAE) animal model to study immune responses associated with multiple sclerosis (MS).
    Myelin basic protein, MBP (68-86)
  • HY-132302
    Hu7691
    		Inhibitor 99.91%
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691
  • HY-N6017
    Bakkenolide A
    		Inhibitor 99.99%
    Bakkenolide A is an anticancer agent. Bakkenolide A reduces the viability of leukemia cells, inhibits cell colony formation and invasion, and downregulates the expression of HDAC3 in cells. Bakkenolide A downregulates the expression of pro-inflammatory cytokines including TNF-α, interleukins such as IL-1β, TGF-β1 and IFN-γ, as well as the expression of PI3K, PDK and PKC in leukemia cells. Bakkenolide A downregulates activated Akt, GSK and Bad, while upregulates Cyto-c, cleaved Caspase3 and cleaved Caspase7, induces apoptosis (apoptosis) in leukemia cells and thereby inhibits inflammatory responses in leukemia cells. Bakkenolide A significantly slows the growth of subcutaneous leukemia tumors in nude mice. Bakkenolide A is applicable to leukemia-related research.
    Bakkenolide A
  • HY-18713A
    CRT0066854 hydrochloride
    		Inhibitor 99.29%
    CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.
    CRT0066854 hydrochloride
  • HY-P5881
    PKCα (C2-4) inhibitor peptide
    		Inhibitor 99.50%
    PKCα (C2-4) inhibitor peptide is a PKCα specific inhibitor peptide that blocks the inhibition of IKr by the α1A adrenoreceptor agonist A-61603 (HY-101366).
    PKCα (C2-4) inhibitor peptide
  • HY-106381A
    Aurothiomalate tetramer sodium
    		Inhibitor 98.0%
    Aurothiomalate tetramer sodium is the tetrameric form of Aurothiomalate sodium (HY-106381). Aurothiomalate tetramer sodium acts as an inhibitor of PKCI and TrxR1. Aurothiomalate tetramer sodium disrupts the PKCI-Par6-Rac1 signaling pathway, and also inhibits TrxR1 activity, TNFα-induced NF-κB activation, and the expression of pro-inflammatory genes. Aurothiomalate tetramer sodium blocks Kras-mediated BASC expansion and lung tumor growth, inhibits anchorage-independent growth and tumorigenicity of lung cancer cells, and suppresses neutrophil chemotaxis, phagocytosis, and leukocyte extravasation. Aurothiomalate tetramer sodium can be used in research related to rheumatoid arthritis and non-small cell lung cancer.
    Aurothiomalate tetramer sodium
  • HY-P5125
    Z-Arg-SBzl
    Z-Arg-SBzl is a substrate of both bovine and activated human protein C.
    Z-Arg-SBzl
  • HY-13866B
    Ro 31-8220 formic
    		Inhibitor 99.76%
    Ro 31-8220 formic 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 formic also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively). Ro 31-8220 formic 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 formic
Cat. No. Product Name / Synonyms Application Reactivity
PKC Isoform Comparison

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