Go 6983 is a PKC inhibitor with IC50 values of 7, 7, 6, 10, and 60 nM for PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, respectively. Go 6983 has antitumor activity, cardiovascular protection, and protein kinase C inhibition.

PKCα:7 nM, PKCμ:20000 nM, PKCγ:6 nM, PKCβ:7 nM, PKCδ:10 nM, PKCζ:60 nM

METHODS: A375, SK-MEL-28, and mouse B16-F10 cells were treated with Go 6983 (0, 0.625, 1.25, 2.5, 5, 10, 20 or 40 μM) for 24, 48, and 72 hours, and the cell growth inhibition was detected by ELISA assay.
RESULTS: The IC50 values of Go 6983, Go 6983 (Go 6983) at 24, 48 and 72 hours were 58.64, 22.07 and 12.93 μM, respectively. [1]

METHODS: To study the antitumor activity of Go 6983, MDA-MB-231 cells or PBS were injected into the humeral metaphysis of each mouse, and 14 days later Go 6983 (2.5 and 5 mg/Kg) was injected intraperitoneally to nude mice for 28 days.
RESULTS: Go 6983 inhibited osteolysis in breast cancer cells. [1]

Phosphorylation reactions are carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HCl, pH 7.5, 10 mM β-mercaptoethanol), 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 μL of a Sf158 cell extract as a source of recombinant PKCμ or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 μg of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [γ-32P]ATP. In some experiments, PS and TPA are omitted or various inhibitors at concentrations indicated in the text are added. After incubation for 10 min at 30°C, the reaction is terminated by transferring 50 μL of the assay mixture onto a 20 mm square piece of phosphocellulose paper, which is washed 3 times in deionized water and twice in acetone. The radioactivity on each paper is determined by liquid scintillation counting.