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

PKCη

PKCη is a novel PKC isoform with predominant epithelial expression and a documented role in cell-cycle control, epithelial junction biology, and immune regulation[1]. Mechanistically, PKCη supports epithelial tight junction integrity by phosphorylating occludin at T403/T404, a finding directly relevant to Caco-2 and MDCK epithelial monolayer models[2]. In keratinocytes, PKCη associates with the cyclin E/CDK2/p21 complex, phosphorylates p21, inhibits CDK2 activity, and promotes G1 arrest[3]. In stress and cancer-cell models, PKCη promotes senescence induced by oxidative stress and DNA damage through p21^Cip1^, p27^Kip1^, IL-6, and IL-6 receptor upregulation, while suppressing IL-8[4]. Compared with related isoforms, PKCη shows isoform-specific biology because different PKCs can exert opposing effects in senescence, and PKCη, rather than PKCθ, controls CTLA-4-mediated regulatory T-cell suppressive function[4][5]. For experimental applications, PKCη studies should prioritize isoform-selective genetic perturbation, phospho-occludin readouts, senescence markers, and CTLA-4-dependent Treg functional assays[2][4][5].

PKCη Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-10230
    Midostaurin
    		Inhibitor 99.89%
    Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
  • HY-18980
    Rottlerin
    		Inhibitor 98.45%
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
  • HY-10343
    Sotrastaurin
    		Inhibitor 99.79%
    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.
  • HY-15727
    Afuresertib
    		Inhibitor 99.53%
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
  • HY-10195
    Ruboxistaurin
    		Inhibitor 99.93%
    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.
  • 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.
  • HY-10195B
    Ruboxistaurin hydrochloride
    		Inhibitor 99.94%
    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.
  • HY-15727A
    Afuresertib hydrochloride
    		Inhibitor 99.95%
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
  • 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.
  • HY-122011
    PF-4950834
    		Inhibitor 99.60%
    PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration.
  • HY-10195A
    Ruboxistaurin mesylate
    		Inhibitor 99.87%
    Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes.
  • HY-143212
    18:0-22:6 DG
    		Activator 99%
    18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (Ki = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease.
  • HY-132302A
    Hu7691 free base
    		Inhibitor
    Hu7691 free base 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 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-124308
    PS315
    		Inhibitor
    PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity.
  • HY-121197
    Balanol
    		Inhibitor
    Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides.
Cat. No. Product Name / Synonyms Application Reactivity