Go 6983 is a pan-PKC inhibitor targeting PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, exhibiting IC50 values of 7 nM, 7 nM, 6 nM, 10 nM, and 60 nM, respectively.

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

22.0 μg i.v. Go6983强烈抑制小鼠肺B16BL6肿瘤模型中51.2 %的肿瘤转移.

Go 6983是靶向作用于ATP结合位点的亚型特异性PKC抑制剂。Go6983抑制ΔPfPKB活性,IC50为1 μM。1 μM Go6983与390 nM Ro-31-8425联用轻微抑制PGSMCs中Angiotensin II诱导的PLD2活性。在Go 6983（5 μM）处理的细胞中,下一个循环中的环数与对照培养物相比明显更少。 Go 6983（5 μM）处理导致恶性疟原虫培养物中新环形成减少近60％。300 μM Go6983抑制转染PKCμ的NIH3T3细胞中PKCμ自磷酸化降低20%。心脏再灌注PMNs和100 nM Go6983,左心室发展压和左心室发展压率分别恢复到基准值的89％和74％,明显高于PMNs单独处理。与心脏缺血再灌注（I/R）+ PMN 相比,100 nM Go6983 PMNs对内皮细胞的粘附和心肌浸润,并显著抑制了PMNs超氧化物释放90％。Go6983在PMNs存在时,降低I/R后心肌收缩功能障碍,这可能与降低超氧化物的产生相关。Go6983明显抑制先前对树花粉致敏的患者的抗原诱导的超氧化物从白细胞释放。Go6983抑制人类血管组织细胞内的Ca(2+)累积,说明其血管舒张特性机制。

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.