| 名稱 | SB 216763 |
| 描述 | SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM). |
| 細(xì)胞實(shí)驗(yàn) | 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(shí)驗(yàn) | 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(guò)對(duì)肺泡上皮細(xì)胞損傷的抑制作用顯著降低博來(lái)霉素誘導(dǎo)的肺泡.在患博來(lái)霉素誘導(dǎo)肺部炎癥和纖維化的小鼠體內(nèi),SB-216763（20 mg/kg）通過(guò)對(duì)炎癥細(xì)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(lái)霉素處理的小鼠壽命. |
| 體內(nèi)活性 | 在人肝臟細(xì)胞中,SB-216763可刺激糖原合成（EC50：3.6 μM）。在HEK293 細(xì)胞在,其可劑量依賴性誘導(dǎo)β-catenin-LEF/TCF相關(guān)報(bào)告基因的轉(zhuǎn)錄,5 μM可誘導(dǎo)達(dá)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(dǎo)的細(xì)胞凋亡,該作用呈濃度依賴性,3 μM時(shí)保護(hù)神經(jīng)達(dá)到最高值。SB-216763（3 μM）可完全抑制LY-294002誘導(dǎo)的雞背根神經(jīng)節(jié)感覺(jué)神經(jīng)元死亡。SB-216763（10 μM）除抑制GSK-3α外,對(duì)糖原合成酶激酶-3也同樣有效（96%）,對(duì)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(xì)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(xì)胞活力,且顯著促進(jìn)凋亡,處理72 h后凋亡達(dá)50%,但不影響HMEC或WI38細(xì)胞系。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% (20% SBE-β-CD in Saline) : < 3.13 mg/mL (8.43 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 31.25 mg/mL (84.18 mM), Sonication is recommended.
10% DMSO+90% Saline : < 3.13 mg/mL (8.43 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+90% Corn oil : < 3.13 mg/mL (8.43 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 3.13 mg/mL (8.43 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
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| 關(guān)鍵字 | SB-216763 | SB 216763 | Inhibitor | inhibit | GSK-3β | GSK-3α | GSK-3 | GSK3 | Glycogen synthase kinase-3 | Glycogen synthase kinase 3 | Autophagy |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Adenosine | Paeonol | Ethyl linoleate |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 神經(jīng)保護(hù)化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 自噬庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 干細(xì)胞分化化合物庫(kù) | 膜蛋白靶向化合物庫(kù) | 免疫/炎癥分子化合物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) |