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-149489
    JH-131e-153
    		Activator
    JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases.
    JH-131e-153
  • HY-101047S1
    D-erythro-Sphingosine-13C2,d2
    		Inhibitor
    D-erythro-Sphingosine-13C2,d2 is a deuterated labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
    D-erythro-Sphingosine-<sup>13</sup>C<sub>2</sub>,d<sub>2</sub>
  • HY-P10471
    MPSD
    MPSD (MARCKS-ED) is a 25-amino acid peptide based on the effector domain sequence of the intracellular membrane protein myristoylated alanine-rich C-kinase substrate (MARCKS). MPSD can sense membrane curvature and recognize phosphatidylserine. MPSD can be utilized as biological probe to study membrane shape and lipid composition.
    MPSD
  • HY-122857
    PKCiota-IN-1
    		Inhibitor
    PKCiota-IN-1 (compound 51) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.7 nM. PKCiota-IN-1 also inhibits PKC-α and PKC-ε with IC50s of 45 nM and 450 nM, respectively.
    PKCiota-IN-1
  • HY-158051
    CIDD-0072424
    		Inhibitor
    CIDD-0072424 selectively inhibits Protein Kinase C-epsilon (PKCε) (Ki=54 nM). CIDD-0072424 reduces ethanol consumption and preference in a dose-dependent manner.
    CIDD-0072424
  • HY-149054
    GSK-3β inhibitor 13
    		Inhibitor
    GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease.
    GSK-3β inhibitor 13
  • HY-117135
    HNS-32
    		Inhibitor
    HNS-32 is a compound with antiarrhythmic and vasodilatory effects in canine hearts, showing superior protective effects against ischemic and reperfusion arrhythmias compared to an equivalent dose of Mexiletine hydrochloride (HY-A0093). Furthermore, HNS-32 exhibits significant negative chronotropic effects on mammalian ventricular myocardium, indicating its potential application value in the study of acute coronary syndrome.
    HNS-32
  • HY-P5452
    PKCd (8-17)
    		Inhibitor
    PKCd (8-17) is a biological active peptide. (This peptide is derived from the V1 domain of protein kinase C (PKC)d. It inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Inhibition of PKCd reduces ischemia damage in cardiac and cerebral cells, induces proliferation of fibroblasts, and inhibits graft coronary artery disease in mice.)
    PKCd (8-17)
  • HY-P5891
    TAT-SAMβA
    		Antagonist
    TAT-SAMβA is the peptide consist of RNAENFDRF (SAMβA; HY-P3429) conjugated to the cell penetrating TAT protein-derived peptide TAT47–57. TAT-SAMβA is a selective antagonist of Mfn1-βIIPKC association. TAT-SAMβA protects mouse embryonic fibroblast cells (MEFs) against oxidative stress-induced cytotoxicity.
    TAT-SAMβA
  • HY-RS11133
    Prkch Rat Pre-designed siRNA Set A
    		Inhibitor

    Prkch Rat Pre-designed siRNA Set A contains three designed siRNAs for Prkch gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Prkch Rat Pre-designed siRNA Set A
    Prkch Rat Pre-designed siRNA Set A
  • HY-P1821
    Myelin Basic Protein
    		98.98%
    Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein 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
  • HY-P3770
    Phosphate acceptor peptide
    		Inhibitor
    Phosphate acceptor peptide is a substrate for cAMP-dependent protein kinase (PKA). phosphate acceptor peptide is also a weak PKC inhibitor.
    Phosphate acceptor peptide
  • HY-P1289B
    [Ala107]MBP(104-118) TFA
    		Inhibitor
    [Ala107]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM.
    [Ala107]MBP(104-118) TFA
  • HY-10195BS
    Ruboxistaurin-d6 hydrochloride
    		Inhibitor
    Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
    Ruboxistaurin-d<sub>6</sub> hydrochloride
  • HY-108603
    Bryostatin 2
    		Control
    Bryostatin 2 ((+)-Bryostatin 2) is a 20-membered ring lactone that can be found in Bryozoan Eugufa neritina L. Bryostatin 2 has the potential for the research of P-388 lymphocytic leukemia.
    Bryostatin 2
  • HY-112291A
    SB 220025 (tri(hydrochloride))
    		Inhibitor
    SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 trihydrochloride also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
    SB 220025 (tri(hydrochloride))
  • 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-N13191
    Ingenol 3-monobenzoate
    		Activator
    Ingenol 3-monobenzoate (Ingenol 3-benzoate) is a disgust inducing agent. Ingenol 3-monobenzoate can bind to and activate PKC (Ki=0.14 nM), inhibit the gene expression of phosphoenolpyruvate carboxykinase, thereby inhibiting gluconeogenesis, and increasing blood cortisol levels, producing food aversion.
    Ingenol 3-monobenzoate
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
PKC Isoform Comparison

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