pkc-in-1

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).

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.

API-1 (NSC-177223) is a potent inhibitor of Akt. It induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis .

ZIP acetate is a novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-ph

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

CaMKII-IN-1, a potent and highly selective inhibitor of CaMKII (IC50 = 63 nM), exhibits over 100-fold higher selectivity for CaMKII compared to CaMKIV, MLCK, p38a, Akt1, and PKC.

R 59-022 (DKGI-I) is a diacylglycerol kinase (DGK) inhibitor and a 5-HT Receptor antagonist that blocks filovirus internalization in host cells. R 59-022 activates protein kinase C (PKC), inhibits intestinal smooth muscle contractility, and enhances O2- production induced by 1-oleoyl-2-acetylglycerol.

HIV-1inhibitor-68 (compound 26) is a derivative that activates protein kinase C (PKC) and exhibits latency-reversing activity in HIV-1. It holds potential for eradicating cells latently infected with HIV-1.

ζ-Stat (NSC37044), a specific and atypical inhibitor of PKC-ζ with an IC50 of 5 μM, demonstrates the ability to inhibit proliferation and induce apoptosis in melanoma cell lines, exhibiting antitumor activity in vitro[1][2].

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

Phosphatidylserine is a phospholipid naturally present in mammals, exhibiting anti-inflammatory and anti-atherosclerotic effects. It activates PKC, neutral sphingolipidase, C-raf-1 protein kinase, and other cofactors involved in multiple signaling pathway activations.

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.

CC-90005 is a potent, selective, and orally active inhibitor of protein kinase C-θ (PKC-θ) with an IC50 of 8 nM, demonstrating strong selectivity over PKC-δ (IC50=4440 nM). Additionally, CC-90005 can inhibit T cell activation by IL-2 expression[1].

Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms that effectively induces the translocation of nPKC-delta, -epsilon, and -theta, as well as PKC-mu, from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].

1,3-Dipalmitin is a diacylglycerol containing palmitic acid at the sn-1 and sn-3 positions. 1,3-Dipalmitin activates protein kinase C α (PKCα) in vitro with a Ka value of 3.8 μM. 1,3-Dipalmitin, at concentrations of 0.25–2 μM, inhibits apoptosis and suppresses the production of reactive oxygen species (ROS) and pro-inflammatory mediators induced by oxygen-glucose deprivation and reperfusion (OGD/R) in SH-SY5Y neuroblastoma cells. 1,3-Dipalmitin is therefore applicable to investigations involving lipid signaling, PKC-associated pathways, neuroinflammation, and ischemia-reperfusion injury models.

Sphingosine (d14:1) is a bioactive sphingolipid that has been found in B. mori (silkworm), P. clarkii (crayfish), and A. aurita (jellyfish) extracts. It increases the germination rate of N. rileyi, an entomopathogenic fungus, with an EC50 value of 10.2 nM. Sphingosine (d14:1) inhibits protein kinase C (PKC) in vitro (IC50 = 7.3 mol%) as well as superoxide generation induced by phorbol 12-myristate 13-acetate in neutrophils and reduces growth of CHO cells (IC50s = 19 and 8 μM, respectively).

Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro. Phellopterin shows a cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM. Phellopterin reduce TNF-alpha-induced VCAM-1 expression through regulation o

1-Oleoyl-2-acetyl-sn-glycerol (1-oleoyl-2-acetyl-glycerol) is a cell-permeable calcium-dependent protein kinase C (PKC) activator that modulates whole-cell Ca2+ currents in a variety of excitable cells and induces the production of superoxide.

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]

1. Nardosinone has inhibitory effect on Ang II-induced hypertrophy in H9c2 cells, might be mediated by targeting PI3K/Akt and MEK/ERK signaling pathways. 2. Nardosinone could protect against the neuronal injury exposed to OGD, which may be relevant to the

PKCiota-IN-1 is a potent inhibitor of PKCiota (PKC-ι), exhibiting an IC50 of 2.7 nM. Additionally, it displays inhibitory activity against PKC-α and PKC-ε, with IC50 values of 45 nM and 450 nM, respectively.

[Ala113]MBP(104-118) TFA is a peptide inhibitor that acts noncompetitively against protein kinase C (PKC), with inhibitory concentrations (IC50) ranging from 28 to 62 μM [1].

Myristoylated TFA Pep2m (Myr-Pep2m TFA) is a cell-permeable peptide that effectively disrupts the interactions between the protein kinase ζ (PKMζ) downstream targets—N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2). PKMζ, an autonomously active isozyme of protein kinase C (PKC), plays a crucial role in these interactions [1] [2].

Malantide TFA, a synthetic dodecapeptide, originates from the phosphorylation site targeted by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Exhibiting a high specificity for PKA with a Michaelis constant (Km) of 15 μM, this compound demonstrates more than 90% inhibition of substrate phosphorylation in the presence of protein inhibitor (PKI) across various rat tissue extracts [1]. Moreover, Malantide TFA acts as an effective substrate for Protein Kinase C (PKC) with a Km of 16 μM [2].