Salubrinal
作者：齊岳
發布時間：2023-08-30
09:00:44
點擊數：
產品名稱：Salubrinal
產品描述：
| 產品描述 | Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α). |
| 靶點活性 | PP1:1.7 μM |
| 體外活性 | 在小鼠角膜感染的模型中,Salubrinal抑制HSV復制,降低感染動物眼拭子中病毒滴度.在腦室內給藥Salubrinal,能夠顯著改變穩態睡眠響應. |
| 體內活性 | Salubrinal（EC50=15 μM）以劑量依賴的方式抑制衣霉素誘導的ER應激,誘導細胞凋亡。Salubrinal（IC50=3 μM）通過抑制eIF2α去磷酸化,而抑制HSV復制。在C12細胞中,Salubrinal下調cyclin D1和上調GADD34和CHOP。 |
| 激酶實驗 | 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]. |
| 細胞實驗 | 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) |
| 分子量 | 479.81 |
| 分子式 | C21H17Cl3N4OS |
| CAS No. | 405060-95-9 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 48 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
