| 名稱 | Go 6983 |
| 描述 | 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 22.0 μg i.v. Go6983強(qiáng)烈抑制小鼠肺B16BL6腫瘤模型中51.2 %的腫瘤轉(zhuǎn)移. |
| 體內(nèi)活性 | Go 6983是靶向作用于ATP結(jié)合位點(diǎn)的亞型特異性PKC抑制劑。Go6983抑制ΔPfPKB活性,IC50為1 μM。1 μM Go6983與390 nM Ro-31-8425聯(lián)用輕微抑制PGSMCs中Angiotensin II誘導(dǎo)的PLD2活性。在Go 6983（5 μM）處理的細(xì)胞中,下一個(gè)循環(huán)中的環(huán)數(shù)與對照培養(yǎng)物相比明顯更少。 Go 6983（5 μM）處理導(dǎo)致惡性瘧原蟲培養(yǎng)物中新環(huán)形成減少近60％。300 μM Go6983抑制轉(zhuǎn)染PKCμ的NIH3T3細(xì)胞中PKCμ自磷酸化降低20%。心臟再灌注PMNs和100 nM Go6983,左心室發(fā)展壓和左心室發(fā)展壓率分別恢復(fù)到基準(zhǔn)值的89％和74％,明顯高于PMNs單獨(dú)處理。與心臟缺血再灌注（I/R）+ PMN 相比,100 nM Go6983 PMNs對內(nèi)皮細(xì)胞的粘附和心肌浸潤,并顯著抑制了PMNs超氧化物釋放90％。Go6983在PMNs存在時(shí),降低I/R后心肌收縮功能障礙,這可能與降低超氧化物的產(chǎn)生相關(guān)。Go6983明顯抑制先前對樹花粉致敏的患者的抗原誘導(dǎo)的超氧化物從白細(xì)胞釋放。Go6983抑制人類血管組織細(xì)胞內(nèi)的Ca(2+)累積,說明其血管舒張?zhí)匦詸C(jī)制。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 22.1 mg/mL (50 mM)
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| 關(guān)鍵字 | G? 6983 | Go 6983 | Go6983 | PKC | inhibit | Go-6983 | Inhibitor | Goe6983 | Goe-6983 | Protein kinase C |
| 相關(guān)產(chǎn)品 | Myricitrin | Midostaurin | Mitoxantrone dihydrochloride | DCPLA-ME | Methyl-Hesperidin | Darovasertib | Staurosporine | R59949 | α-Vitamin E | Ro-3306 | Daphnetin | N-Desmethyltamoxifen hydrochloride |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 抗心血管疾病化合物庫 | 抗衰老化合物庫 | 細(xì)胞骨架化合物庫 | 干細(xì)胞分化化合物庫 | TGF-β/Smad靶點(diǎn)化合物庫 | 細(xì)胞重編程化合物庫 |