pkcα

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.

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.

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

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).

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

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.

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.

Ingenol 3-monobenzoate (Ingenol 3-benzoate) acts as an aversive inducing agent. It binds to and activates protein kinase C (PKC) with a Ki of 0.14 nM. This activation inhibits the gene expression of phosphoenolpyruvate carboxykinase, thereby suppressing gluconeogenesis and increasing blood cortisol levels, which results in food aversion.

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.

Prostratin (12-Deoxyphorbol-13-acetate) is an orally active protein kinase C (PKC) activator with a Ki value of 12.5 nM.As an NF-κB activator, Prostratin activates HIV gene expression in T cells.Prostratin inhibits the growth of acute myeloid leukemia (AML) cell lines and enhances cytarabine-induced AML cell differentiation. In addition, Prostratin induced KRAS phosphorylation and inhibited the growth of KRAS-mutated tumors.

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.

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.

1,2-Dipalmitoyl-sn-glycerol ((S)-1,2-Dipalmitin) is an analog of the PKC-activating second messenger diacylglycerol (DAG). It weakly activates PKC.

1,2-Dimyristoyl-sn-glycerol (1,2-DMG) is able to increase AChE activity by 35-40% at concentrations of 25 micrograms ml in the parasite S. mansoni..

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

Coniferaldehyde (Ferulaldehyde) is a member of the class of cinnamaldehydes that is cinnamaldehyde substituted by a hydroxy group at position 4 and a methoxy group at position 3. It has a role as an antifungal agent and a plant metabolite. It is a member of cinnamaldehydes, a phenylpropanoid and a member of guaiacols. It derives from a cinnamaldehyde.

Balanol is an ATP-competitive Protein Kinase C and Protein Kinase A inhibitor.

Leucosceptoside A is a compound isolated from the bark of Oroxylum indicum, with antidiabetic and antihypertensive properties. It modulates psoriasis-like inflammation by inhibiting the PI3K AKT pathway in keratinocytes.

Licarin A is a natural anti-inflammatory lignan that inhibiting PKCα βII and p38 MAPK pathways, thereby decreasing TNF-α and prostaglandin D2 (PGD2) secretion as well as COX-2 expression.

1. Decursin (Decursinol angelate) is able to attenuate kainic acid-induced seizures and could have potential as an antiepileptic drug. 2. Decursin exhibits hepatoprotective effects , potentially by inhibiting the TGF-β1 induced NOX activation and Smad signaling. 3. Decursin has anti-cancer activity , mediated suppression of the PKCα, MAPK and NF-κB pathways in MCF-7 cells. 4. Decursin exhibits cytotoxicity against various human cancer cells and to possess anti-amnesic activity in vivo through the inhibition of AChE activity.

Ingenol mebutate (Ingenol 3-Angelate) is a potent activator of PKC subtypes including PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM. Ingenol mebutate exhibits antiinflammatory and antitumor activity.