protein kinase c

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

Ionomycin calcium (SQ23377 calcium) is an effective and selective calcium ionophore, demonstrating high specificity for divalent cations (Ca>Mg>Sr=Ba).

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

D-erythro-Sphingosine (trans-4-Sphingenine) is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

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.

Hypocrellin A is a natural PKC inhibitor with light-induced antitumor, antifungal and antiviral activities and also exerts immunomodulatory effects on MHC-restricted antigen presentation.

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

Ionomycin is an calcium ionophore and an antibiotic that binds calcium ions (Ca2+). It is produced by the bacterium Streptomyces conglobatus.It is used in research to raise the intracellular calcium level (Ca2+) and as a research tool to understand Ca2+ transport across biological membranes. Ionomycin promotes apoptosis and induces the activation of protein kinase C (PKC).

Artemisinin (Qinghaosu) is a natural product, a sesquiterpene lactone, derived from Artemisia annua. Artemisinin has anti-malarial activity, as well as neuroprotective and anti-tumor activity.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1 ERK2.

Cholesteryl sulfate sodium (Sodium Cholesteryl Sulfate) is a sterol sulfate in human plasma. Cholesteryl sulfate sodium is a component of cell membrane and has a regulatory function. Cholesteryl sulfate sodium also activates multiple protein kinase C (PKC) iso-enzymes, especially the ε, η and ζ isoforms.

Methyl cinnamate, a tyrosinase inhibitor and a flavoring compound, has antimicrobial, antiadipogenic, vasorelaxant, and anti-inflammatory effects.

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. Isolated from hyssop oil, it possesses antifungal, highly active whitening, and antioxidant properties, and it has potential applications in cosmeceutical materials. It downregulates proinflammatory cytokines in vitro and in vivo, reduces the number of total cells, neutrophils, and macrophages in BALF, attenuates histologic lung alterations, decreases the wet-to-dry weight ratio in BALF, and inhibits the activation of NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, and p38 mitogen-activated protein kinase.

Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10 30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

10-Gingerol-induced apoptosis was accompanied by phosphorylation of the mitogen-activated protein kinase (MAPKs) family, p38 MAPK (p38), c-Jun N-terminal kinase (JNK), and extracellular signal-regulated kinase (ERK).

1. Vitexin has antinociceptive and antispasmodic activities. 2. Vitexin exhibits a prominent first-pass effect. 3. Vitexin has antioxidant, antimyeloperoxidase, and α-glucosidase inhibitory activities. 4. Vitexin can either inhibit or induce activities of

Hispidin is a natural product, protein kinase C inhibitor, which belongs to the group of 2-pyrones and catechols. It has anti-inflammatory activity, anti-cancer activity, inhibition of oxidative stress and anti-apoptosis.

Palmitoylcarnitine chloride (Palmitoyl DL-carnitine chloride) is a mitochondrial fatty acid oxidation intermediate that mediates intralipid cardioprotection.Palmitoylcarnitine chloride eliminates colorectal cancer cell survival by depletion of glutathione. induces cancer cell death and regulates the interaction between protein kinase C βII and its receptor RACK1.

K-252b, an indolocarbazole derived from the actinomycete Nocardiopsis, functions as a protein kinase C (PKC) inhibitor. It is effective in inhibiting extracellular kinases in cultured cells due to its inability to freely cross the cell membrane.

Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II.