化合物SC 79 T2274

Product Introduction
Bioactivity


英文名: SC79

描述: SC79 是一个 AKT 激动剂，具有特异性和血脑屏障渗透性。SC79 可以特异性结合 AKT 的 PH 结构域，激活胞质中 AKT，并抑制 AKT 膜转位。SC79 具有神经保护活性。

细胞实验: HsSultan or NB4 cells (2.5 × 105) are plated in a 24-well plate in 500 μL of phenol red-free RPMI medium supplemented with 10% FBS. After incubation for 24 hours, each compound (8 μg/mL) is added and cultured for overnight (16–20 h). Fifty microliters of MTT solution (5 mg/mL in PBS) are added to each well. Following 2 hrs incubation, the purple formazan crystals are dissolved by directly adding in 500 μL of isopropanol with 0.1 M HCl to each well. After clearing the cell debris by centrifugation, the absorbance is measured at a wavelength of 570 nm.(Only for Reference)

激酶实验: Cytosolic phosphorylation of Akt: Hela cells are serum starved for 1 hr and treated with IGF (100ng/mL) or SC79 (4 μg/mL) for 30 minutes. Cells are lysed in Lysis buffer containing 250 mM Sucrose, 20 mM HEPES, 10 mM KCl, 1.5 mM MgCl2, 1 mM EDTA, 1 mM EGTA supplemented with protease inhibitors. Cells are passed through 25 g needle several times and kept on ice for 20 minutes. Total cell lysate is taken at this point. Cell lysates are centrifuged at 100,000 g for 30 minutes. Supernatant is collected as the cytosolic fraction. Pellet is washed with lysis buffer and represents the membrane fraction. Total cell lysate, cytosolic and membrane fractions are resolved by SDS-PAGE and analyzed for phospho-Akt (S473), Total Akt, Tubulin (cytosolic marker) and Orai1 (membrane marker) by western blotting.

体外活性: 方法：人宫颈癌细胞 HeLa 血清饥饿 1 h，用 SC79 (4 µg/mL) 处理 30 min，使用 Western Blot 检测靶点蛋白表达水平。结果：SC79 增强了 AKT 磷酸化，SC79 诱导的 AKT 磷酸化主要发生在胞质中。[1]方法：人肺癌细胞 A549 用 SC79 (10 µg/mL) 处理 24 h，使用 qPCR 检测基因表达水平。结果：SC79 处理上调了 Nrf-2 (NFE2L2) 基因本身以及下游靶标 HO-1 和 NQO-1 的表达。[2]

体内活性: 方法：为检测体内活性，将 SC79 (0.04 mg/g) 腹腔注射给 C57 Black/6 小鼠铜松脱髓鞘模型，5 min 后进行大脑中动脉闭塞 (MCAO) 构建缺血性中风模型。结果：单次剂量的 SC79 在 MCAO 后 24 h 和 MCAO 后 1 周将新皮质病变的大小分别减少 35% 和 40% 以上。[1]方法：为研究对肝损伤的作用，将 SC79 (10 mg/kg) 腹腔注射给 C57BL/6 小鼠，0.5 h 后注射 d-Gal/LPS 诱导肝损伤。结果：SC79 保护小鼠免受 d-Gal/LPS 诱导的 TNF-α 介导的肝损伤。[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (150.78 mM)
5% DMSO+95% Saline : 1.83 mg/mL (5 mM, suspension)


关键字: inhibit | Akt | Protein kinase B | SC79 | Inhibitor | SC-79 | PKB

相关产品: Chromeceptin | Icariside B1 | Eupatolide | 2,3-Dihydro-3-methoxywithaferin A | AKT Kinase Inhibitor | Kihadanin B | Bakkenolide IIIa | Kanosamine hydrochloride | Scutellarin | GSK-690693

相关库: Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Cancer Compound Library | Glutamine Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Kinase Inhibitor Library | Metabolism Compound Library | Glycolysis Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途