PKC

chemotherapy drug used to treat bladder cancer

Pan-PKC inhibitor

negative control for protein kinase C (PKC)-inhibitory activity

(-)-epigallocatechin is a major polyphenolic compound in green tea with antioxidant properties.

A protein kinase G inhibitor

Protein kinase C activator

Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM).

D-erythro-Sphingosine (synthetic) is a bioactive activator of p32 kinase (EC 50 =8μM).

PKC activator

Non-competitive inhibitor of PKC

Dihydrosphingosine is a potent inhibitor of PKC and phospholipase A2 (PLA2).

L-threo-Sphingosine C-18 is a potent MAPK inhibitor. L-threo-Sphingosine C-18 induces apoptosis and clear DNA fragmentation. L-threo-Sphingosine C-18 shows anticancer effect.

protein kinase C activator

A longchain DAG

R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate.

Bisindolylmaleimide X (hydrochloride) is a novel, cell-permeable protein kinase C (PKC) inhibitor. Bisindolylmaleimide X also inhibits cyclin-dependent kinase 2 (CDK2) activity.

Cercosporin is a pigmented phytotoxin isolated from the fungus C.

N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC).

WAY-354831 exhibits antibacterial activity.

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

Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.

Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.

PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.