| 名稱 | SB 216763 |
| 描述 | SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM). |
| 細胞實驗 | Cells are exposed to various concentrations of SB 216763 for 24, 48 and 72 hours. Relative cell viability is measured using the MTS assay. Apoptotic cells are determined by staining with Hoechst.(Only for Reference) |
| 激酶實驗 | GSK-3 activity assay: GSK-3 kinase activity is measured, in the presence of various concentrations of SB 216763, in a reaction mixture containing final concentrations of 1 nM human GSK-3α, 50 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM Mg-acetate, 7.5 mM β-mercaptoethanol, 5% (w/v) glycerol, 0.01% (w/v) Tween-20, 10% (v/v) DMSO, and 28 μM GS-2 peptide substrate. The GS-2 peptide sequence corresponds to a region of glycogen synthase that is phosphorylated by GSK-3. The assay is initiated by the addition of 0.34 μCi [33P]γ-ATP. The total ATP concentration is 10 μM. Following 30 minutes incubation at room temperature the assay is stopped by the addition of one third assay volume of 2.5% (v/v) H3PO4 containing 21 mM ATP. Samples are spotted onto P30 phosphocellulose mats and washed six times in 0.5% (v/v) H3PO4. The filter mats are sealed into sample bags containing Wallac betaplate scintillation fluid. 33P incorporation into the substrate peptide is determined by counting the mats in a Wallac microbeta scintillation counter. |
| 體外活性 | SB-216763通過對肺泡上皮細胞損傷的抑制作用顯著降低博來霉素誘導的肺泡.在患博來霉素誘導肺部炎癥和纖維化的小鼠體內(nèi),SB-216763（20 mg/kg）通過對炎癥細胞因子MCP-1和TNF-α產(chǎn)量的顯著抑制作用,從而明顯抑制肺部炎癥和纖維化,且明顯提高用博來霉素處理的小鼠壽命. |
| 體內(nèi)活性 | 在人肝臟細胞中,SB-216763可刺激糖原合成（EC50：3.6 μM）。在HEK293 細胞在,其可劑量依賴性誘導β-catenin-LEF/TCF相關(guān)報告基因的轉(zhuǎn)錄,5 μM可誘導達到最大值（增大2.5倍）。在小腦顆粒神經(jīng)元中,SB-216763可使之免受LY-294002或鉀喪失誘導的細胞凋亡,該作用呈濃度依賴性,3 μM時保護神經(jīng)達到最高值。SB-216763（3 μM）可完全抑制LY-294002誘導的雞背根神經(jīng)節(jié)感覺神經(jīng)元死亡。SB-216763（10 μM）除抑制GSK-3α外,對糖原合成酶激酶-3也同樣有效（96%）,對其余24種蛋白激酶包括PKBα和PDK1的活性很?。↖C50>10 μM）。在前列腺癌細胞系,包括MIA-PaCa2,BXPC-3,PANC1,ASPC1和CFPAC中,SB-216763（25-50 μM）可劑量依賴性降低細胞活力,且顯著促進凋亡,處理72 h后凋亡達50%,但不影響HMEC或WI38細胞系。 |
| 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 : 10 mg/mL (26.94 mM), Sonication is recommended.
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| 關(guān)鍵字 | SB-216763 | GSK-3 | Autophagy | Inhibitor | Glycogen synthase kinase 3 | inhibit | Glycogen synthase kinase-3 | SB 216763 |
| 相關(guān)產(chǎn)品 | Oxyresveratrol | Guanidine hydrochloride | Naringin | Taurine | Gefitinib | Xylitol | Hydroxychloroquine | Curcumin | Stavudine | Myricetin | Paeonol | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 抑制劑庫 | 神經(jīng)保護化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 氧化還原化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 抗肺癌化合物庫 | 糖代謝化合物庫 | 神經(jīng)退行性疾病化合物庫 |