| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Preparation Method | Phosphorylation reactions were carried out in a total volume of 100 μl, containing buffer C, 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 ul of a Sf158 cell extract as a source of recombinant PKCu or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 ug of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [y-32P] ATP. In some experiments PS and TPA were omitted or various inhibitors(including Go 6983 (Go 6983)) at concentrations were added. After incubation for 10 min at 30℃, the reaction was terminated by transferring 50 ul of the assay mixture onto a 20 mm square piece of phosphocellulose paper (Whatman p81), which was washed 3 times in deionized water and twice in acetone. |
Reaction Conditions | 10-1-106nM Go 6983 (Go 6983) for 10 min at 30℃ |
Applications | Go 6983 (Go 6983) is a pan-PKC inhibitor that acts on PKCα, PKCβ, PKCγ and PKCδ with IC50 values of 7 nM, 7 nM, 6 nM and 10 nM, respectively. Go 6983 (Go 6983) has a weak effect on PKCζ and inhibits the activity of PKCμ. |
Cell lines | MDA-MB-231 cells |
Preparation Method | MDA-MB-231 cells were seeded in 96-well plates and incubated overnight. Next, various concentrations of Go 6983 (Go 6983) (0, 0.625, 1.25, 2.5, 5, 10, 20, or 40 μM) were added to the cells to incubate for 24, 48 and 72 h. PMS (100 μL) and MTS (2 mL) were thoroughly mixed, and the resulting solution was added to each well of the 96-well plate. Finally, the optical density (OD) at 490 nm of each well was measured by using an enzyme-linked immunosorbent assay (ELISA) plate reader. |
Reaction Conditions | Go 6983 (Go 6983) (0, 0.625, 1.25, 2.5, 5, 10, 20, or 40 μM) for 24, 48 and 72 h |
Applications | The IC50 of Go 6983 (Go 6983) at 24, 48, and 72 h were 58.64, 22.07, and 12.93 μM, respectively.At the concentrations used in our experiments, Go 6983 (Go 6983) has no toxic effects on MDA-MB-231 cells. Go 6983 (Go 6983) inhibits invasion and migration of MDA-MB-231 cells. |
Animal models | Nude mice |
Preparation Method | Twenty-four nude mice were divided randomly into the following four groups: Sham group, vehicle group, low dose group, and high dose group. MDA-MB-231 cells or PBS were injected into the humeral metaphysis of each mouse. After 14 days, the mice in the vehicle and sham groups were injected intraperitoneally with 100 μL of PBS, and high- and low-dose groups were injected intraperitoneally daily with 5 or 2.5 mg/kg Go 6983 (Go 6983), respectively. All mice were sacrificed 28 days later, and tumor growth and bone destruction were observed by X-ray and microCT. The tumor tissues were examined histologically, and the long diameter, short diameter, and volume of the tumor were measured. |
Dosage form | 5 or 2.5 mg/kg Go 6983 (Go 6983) for 28days |
Applications | Go 6983 (Go 6983) can inhibit breast cancer osteolysis in vivo. |
| 产品描述 | Go 6983 (GO 6983) is one of the bisindolylmaleimide group of PKC inhibitor compounds, Go 6983 (GO 6983) was able to differentiate between PKC mu and other PKC isoenzymes. Go 6983 (GO 6983) is a pan-PKC inhibitor that acts on PKCα, PKCβ, PKCγ and PKCδ with IC50 values of 7 nM, 7 nM, 6 nM and 10 nM, respectively. Go 6983 (GO 6983) has a weak effect on PKCζ and inhibits the activity of PKCμ[3,4]. Go 6983 (GO 6983) inhibits invasion and migration of MDA-MB-231 cells. Go 6983 (GO 6983) activates the mitochondrial apoptosis pathway in MDA-MB-231 cell. Go 6983 (GO 6983) inhibits the Src pathway in MDA-MB-231 cells and inhibits phosphorylation of PKC[2]. Platelet aggregation induced by epi was potentiated by RO 31-8220 (RO) or Go 6983 (GO 6983)[1]. Go 6983 (GO 6983) may exert cardioprotection by en- hancing endothelial NO release, which has been found to be cardioprotective in the setting of MI/R[6]. Tumor volume, long diameter, and short diameter were all lower in the mice injected with Go 6983 (GO 6983) than in those of the vehicle control group (Figures 1B D). The volume of tumors in the high dose group was approximately one-third of those in the vehicle group, indicating that Go 6983 (GO 6983) suppresses the growth and bone metastasis of breast cancer[2]. Go 6983 (GO 6983) (100 nM) significantly reduced PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts, and significantly inhibited superoxide release from PMNs. In the presence of PMNs, Go 6983 (GO 6983) attenuated post-I/R cardiac contractile dysfunction, which may be related in part to decreased superoxide production[5]. Go 6983 (GO 6983) was able to attenuate urotensin II-induced contraction in rat aorta, in this case, through inhibition of Ca 2+/calmodulin/MLC kinase[7]. References: |
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