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-N7144A
    Citronellyl acetate
    		98.0%
    Citronellyl acetate, a monoterpene product of the secondary metabolism of plants, is an orally active antinociceptive agent. Citronellyl acetate modulates TRPV1, TRPM8, ASIC, glutamate receptors, PKC, and PKA-mediated nociception. Citronellyl acetate can be used for the research of acute pain.
    Citronellyl acetate
  • HY-15141G
    Staurosporine (GMP)
    		Inhibitor
    Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases.
    Staurosporine (GMP)
  • HY-15141R
    Staurosporine (Standard)
    		Inhibitor
    Staurosporine (Standard) is the analytical standard of Staurosporine. This product is intended for research and analytical applications. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC50 of 3 μM. Staurosporine is an apoptosis inducer[1][2][3][4][5].
    Staurosporine (Standard)
  • HY-N4246
    Bacopaside I
    		Modulator 99.20%
    Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases.
    Bacopaside I
  • HY-128142
    PKC/PKD-IN-1
    		Inhibitor 98.35%
    PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC50 value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure.
    PKC/PKD-IN-1
  • HY-13661
    7-Hydroxystaurosporine
    		Inhibitor
    7-Hydroxystaurosporine (UCN-01), a derivative of Staurosporine (HY-15141), is a selective protein kinase C (PKC) inhibitor with antitumor activity. 7-hydroxystaurosporine induces apoptosis and inhibits cell proliferation in colon carcinoma and leukemia cells, suppresses invasion and migration in glioblastoma cells. 7-Hydroxystaurosporine exhibits efficacy in breast cancer xenograft mouse models. 7-Hydroxystaurosporine can be used for colon carcinoma, breast cancer, glioblastoma and leukemia research.
    7-Hydroxystaurosporine
  • HY-101810
    Tazanolast
    		Inhibitor 99.50%
    Tazanolast (TO 188) is an orally active selective mast cell stabilizer. Tazanolast prevents the elevation of intracellular calcium concentration, inhibits calcium uptake and Protein kinase C translocation, without directly inhibiting phospholipase C. Tazanolast inhibits ozone-induced airway hyperresponsiveness to Methacholine in guinea pigs, as well as passive cutaneous anaphylaxis, Schultz-Dale reaction, experimental asthma, passive cutaneous anaphylaxis in rats, and increased cutaneous vascular permeability in rats. Tazanolast does not alter airway responsiveness in sham-exposed guinea pigs, cell distribution in bronchoalveolar lavage fluid after ozone exposure, type II-IV allergic reactions, or histamine release from atopic leukocytes. Tazanolast can be used in research related to allergic diseases.
    Tazanolast
  • HY-P3429A
    SAMβA TFA
    		Inhibitor 99.13%
    SAMβA TFA is a rationally designed selective antagonist of Mfn1-βIIPKC association and can bind to TAT (HY-P0281). SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats.
    SAMβA TFA
  • HY-122246
    ML192
    		Inhibitor 99.70%
    ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.
    ML192
  • HY-122858A
    PKCiota-IN-2 formic
    		Inhibitor 99.04%
    PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 formic also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
    PKCiota-IN-2 formic
  • HY-164756
    PKCTheta-IN-2
    		Inhibitor 99.49%
    PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor with an IC50 of 0.25 nM. PKCTheta-IN-2 shows good selectivity over a wide range of kinases, including the PKC subfamily (30 kinases). PKCTheta-IN-2 inhibits the IL-2 production in a mouse (IC50 of 682 nM).
    PKCTheta-IN-2
  • HY-123979A
    ζ-Stat trisodium
    		Inhibitor
    ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
    ζ-Stat trisodium
  • HY-P3012
    Cathepsin G
    		Activator
    Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases.
    Cathepsin G
  • HY-117393
    Bisindolylmaleimide III
    		Inhibitor 98.95%
    Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases.
    Bisindolylmaleimide III
  • HY-P1399A
    Pep2m, myristoylated TFA
    		Inhibitor 99.77%
    Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC).
    Pep2m, myristoylated TFA
  • HY-107207
    Kaempferol 3-neohesperidoside
    		Modulator 99.68%
    Kaempferol 3-neohesperidoside (Kaempferol 3-O-neohesperidoside) is a flavonoid. Kaempferol 3-neohesperidoside mimics insulin action via the PI3K/PKC pathway, significantly promoting glucose uptake and increasing muscle glycogen content in rat soleus muscles. Kaempferol 3-neohesperidoside also exhibits anti-glycation activity. Kaempferol 3-neohesperidoside binds to albumin through hydrogen bonding and hydrophobic interactions, and inhibits the formation of advanced glycation end products. Kaempferol 3-neohesperidoside can be used in studies of diabetes and its related complications.
    Kaempferol 3-neohesperidoside
  • HY-N0453R
    Hypericin (Standard)
    		Inhibitor
    Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.
    Hypericin (Standard)
  • HY-N1400
    (20R)-Ginsenoside Rh1
    		99.94%
    (20R)-Ginsenoside Rh1 is the R-isomer of Ginsenoside Rh1 (HY-N0604), and it is found in red ginseng, ginseng, and other sources. (20R)-Ginsenoside Rh1 inhibits thrombin-induced conversion of fibrinogen to fibrin, exerting anticoagulant and antithrombotic effects.
    (20R)-Ginsenoside Rh1
  • HY-112465
    H-8 dihydrochloride
    		Inhibitor 99.19%
    H-8 dihydrochloride is a selective Cyclic nucleotide-dependent protein kinase inhibitor. H-8 dihydrochloride potently inhibits cGMP- and cAMP-dependent protein phosphorylation. H-8 dihydrochloride enhances the vasodilatory effect induced by 8-bromo-cAMP (HY-12306A). H-8 dihydrochloride fails to attenuate the vasodilatory effects induced by 8-bromo-cGMP (HY-101379A), atrial natriuretic peptide II, or Sodium nitroprusside (HY-B0564) in rat aorta.
    H-8 dihydrochloride
  • HY-P1746
    Protein Kinase C (19-31)
    		Inhibitor 99.74%
    Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31), is used as protein kinase C substrate peptide for testing the protein kinase C activity.
    Protein Kinase C (19-31)
Cat. No. Product Name / Synonyms Application Reactivity
PKC Isoform Comparison

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