| 名稱 | Salubrinal |
| 描述 | Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α). |
| 細(xì)胞實(shí)驗(yàn) | PC12 cells are plated in 384-well plates at 5000 cells per well in 40μL phenol red-freemedium containing 3μg/ml Tm to induce ER stress. 100 nL of the DiverSet E (5 mg/mlin DMSO) or National Cancer Institute's (NCI) Structural Diversity set and Open Collections (10 mM in DMSO) (NCI) are added to the wells by robotic pin transfer. After 48 hours, cell viability is assessed using a luminescence-based ATP assay. DMSO- and zVAD.fmk-treated wells on each plate served as negative and positive controls for rescue from ER stress-induced ATP loss, respectively.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Phosphatase activities are determined on immunoprecipitates of the phosphatases. Briefly, 2×106 K562 cells are treated for 18 hr with Salubrinal (20 μM), PSI (10 nM), the combination of both drugs or okadaic acid (100 nM). After washing with PBS, cells are lysed for 15 min on ice either in PP1LB (for determination of PP1γ-activity; 20 mM Tris-HCl, pH 7.5, 1% Triton X-100, 10% glycerol, 132 mM NaCl, Roche complete protease inhibitor ) or in RIPA (for PP2A), supplemented with Roche complete protease inhibitor). Cell lysates containing 500 μg (PP1γ) or 300 μg (PP2A) protein are immunoprecipitated overnight at 4°C with 2-3 μg of the appropriate antibodies and then incubated with Protein A-Sepharose. Immunoprecipitates are washed three times in lysis buffer, followed by resuspension in phosphatase assay buffer (PP2A: 20 mM Tris-HCl, pH7.5, 0.1 mM CaCl2; PP1γ: 50 mM Tris HCl pH 7.0, 0.2 mM MnCl2, 0.1 mM CaCl2, 125 μg/mL BSA, 0.05% Tween 20), supplemented with 100 μM 6,8-difluoro-4-methyl-umbelliferyl phosphate (DiFMUP). Precipitates are allowed to react with substrate for 1 hr at 37°C on an Eppendorf Thermoshaker, centrifuged and DiFMU fluorescence is measured on a BioTek Lambda Fluoro 320 microplate reader (360 nmex/460 nmem). Phosphatase activities are given as percent change relative to the control (DMSO treated cells)[1]. |
| 體外活性 | 在小鼠角膜感染的模型中,Salubrinal抑制HSV復(fù)制,降低感染動(dòng)物眼拭子中病毒滴度.在腦室內(nèi)給藥Salubrinal,能夠顯著改變穩(wěn)態(tài)睡眠響應(yīng). |
| 體內(nèi)活性 | Salubrinal（EC50=15 μM）以劑量依賴的方式抑制衣霉素誘導(dǎo)的ER應(yīng)激,誘導(dǎo)細(xì)胞凋亡。Salubrinal（IC50=3 μM）通過抑制eIF2α去磷酸化,而抑制HSV復(fù)制。在C12細(xì)胞中,Salubrinal下調(diào)cyclin D1和上調(diào)GADD34和CHOP。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 40 mg/mL (83.37 mM)
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| 關(guān)鍵字 | Autophagy | Herpes simplex virus | Salubrinal | HSV | Phosphatase | Apoptosis | Inhibitor | inhibit |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Stearic acid | Taurine | Gefitinib | Hydroxychloroquine | Curcumin | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate |
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