pkcε

PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).

PKCε Inhibitor Peptide acetate is a selective PKCε inhibitor containing the site for its specific receptor for activated C kinase (RACK). PKCε Inhibitor Peptide acetate inhibits the translocation of PKCε, but not α-, β-, and δPKC.

DCPLA-ME (2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester) is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.

Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, exerts antinociceptive effects.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

DCP-LA (FR236924), linoleic acid derivatives, selective and direct activation of PKCε.

AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

(-)-Indolactam V, a potent PKC activator, exhibits binding affinities (Kis) of 3.36 nM and 1.03 μM for η-CRD2 and γ-CRD2, respectively, and dissociation constants (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), and 213 nM (γ-C1B), also demonstrating antitumor activity.

Epsilon-V1-2 has been extensively investigated for its function as a PKC epsilon (PKCε) inhibitor. Epsilon-V1-2 has been widely applied in studies addressing ovarian aging, apoptosis in human granulosa cells, cerebral ischemia-reperfusion injury, brain development, hepatocyte insulin signaling, and neuronal cell death under ischemic conditions. Epsilon-V1-2 has been shown to effectively reduce PKCε activity, thereby enabling detailed exploration of regulatory pathways involving mitochondrial dynamics, calcium overload, AKT activation, brain atrophy, insulin resistance, and ferroptosis. Epsilon-V1-2 demonstrates notable therapeutic relevance in models of stroke, SHORT syndrome, hepatic steatosis, and brain injury, supporting its continued evaluation as a potential pharmacological agent across multiple disease contexts.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

Enzastaurin (LY317615) (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε.

Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.

PKCε (85-92) (ψεRACK) is a peptide and selective PKCε activator that does not affect the activity of other PKC isozymes.PKCε (85-92) induces a pro-angiogenic response in endothelial cells, promotes FGF-2 cytosolization, and regulates VEGF activity.

Myristoylated PKCε inhibitor peptide (Myr-PKCε-) is a cell-permeable inhibitor consisting of a peptide linked to myristic acid that specifically inhibits protein kinase C epsilon (PKCε), consequently diminishing nitric oxide (NO) release in cultured human umbilical vein endothelial cells (HUVECs) [1].

PKC β pseudosubstrate acetate (PKC β pseudosubstrate acetate (172308-76-8 Free base)) is a selective cell-permeable inhibitor of PKC.

PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)

PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor (IC50 = 0.25 nM) that suppresses IL-2 production in mice (IC50 = 682 nM).

PKC-IN-5 (Compound PKCe2054) is a protein kinase C (PKC) inhibitor that disrupts the interaction between PKCe and its anchoring protein RACK2.

PKC-IN-7 is an inhibitor of PKC and can be utilized in research related to diseases such as cancer.

PKC-theta inhibitor is PKC-θinhibitor, with an IC50 of 12 nM.

PKC-theta inhibitor hcl is a selective PKC-θinhibitor(IC50:12 nM).

PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), with an IC 50 value of 0.52 µM. In vitro studies show that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α and impedes retinal vasculature permeability induced by both VEGF and TNF-α. [1]

Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, θ), exhibiting inhibitory activity on AurA (IC50: 6.9 nM) and PKCα (IC50: 16.9 nM), and demonstrating anti-proliferative and anti-metastatic effects on breast cancer cells.