Chelerythrine is a Potent Protein kinase C Inhibitor
Chelerythrine is a natural benzo[c]phenanthridine alkaloid. It extracts from a number of plant species, such as Chelidonium majus, Macleaya cordata, Sanguinaria canadensis, etc. This compound exerts a wide spectrum of biological activities, including anti-cancer, anti-diabetes, anti-fungus, as well as a protective effect against the ethanol-induced gastric ulcer and the...
Staurosporine is an ATP-competitive Inhibitor of Protein Kinases
Protein kinases are enzymes that catalyze protein phosphorylation. Obviously, Protein kinases include many types of kinases, such as PKC，PKA, c-Fgr and phosphorylase kinase. Thereinto, PKC, PKA and phosphorylase kinase belong to serine or threonine kinases and c-Fgr belongs to Tyr kinases. Interestingly, diacylglycerol (DG) can activate PKC and the...
R59949 is a pan Diacylglycerol Kinase (DGK) Inhibitor
Diacylglycerol kinase (DGK) is a second messenger in its own right and can modulate the activity of PKC and several ion channels. Chemokines are low MW extracellular signaling peptides secreted by tissue either constitutively during homeostasis or de novo during an inflammatory response. They are a diverse family of...
PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket
Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...
BJE6-106, a Selective PKCδ Inhibitor, Triggers Caspase-Dependent Apoptosis
Melanomas were responsible for more than 75% of estimated skin cancer deaths in 2012. And the incidence rate has been increasing for the last 30 years. Additionally, NRAS is the second most frequently mutated gene in melanoma. Researcheres also have demonstrated the sensitivity of cancer cell lines carrying KRAS...