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SC79

SC79

产品编号 T2274   CAS 305834-79-1
别名: SC 79, 2-氨基-6-氯-alpha-氰基-3-(乙氧羰基)-4H-1-苯并吡喃-4-乙酸乙酯

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。

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SC79 Chemical Structure
SC79, CAS 305834-79-1
规格 价格/CNY 货期 数量
1 mg ¥ 215 现货
5 mg ¥ 472 现货
10 mg ¥ 763 现货
25 mg ¥ 1,380 现货
50 mg ¥ 2,320 现货
100 mg ¥ 3,480 待询
200 mg ¥ 4,730 待询
1 mL * 10 mM (in DMSO) ¥ 472 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: SC79 (T2274)
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纯度: 100%
纯度: 98%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SC79 is an AKT agonist with specificity and blood-brain barrier permeability. SC79 specifically binds to the PH domain of AKT, activates cytoplasmic AKT, and inhibits AKT membrane translocation. SC79 has neuroprotective activity.
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]
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.
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)
别名 SC 79, 2-氨基-6-氯-alpha-氰基-3-(乙氧羰基)-4H-1-苯并吡喃-4-乙酸乙酯
分子量 364.78
分子式 C17H17ClN2O5
CAS No. 305834-79-1

存储

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

溶解度

DMSO: 36.5 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7414 mL 13.7069 mL 27.4138 mL 68.5345 mL
5 mM 0.5483 mL 2.7414 mL 5.4828 mL 13.7069 mL
10 mM 0.2741 mL 1.3707 mL 2.7414 mL 6.8534 mL
20 mM 0.1371 mL 0.6853 mL 1.3707 mL 3.4267 mL
50 mM 0.0548 mL 0.2741 mL 0.5483 mL 1.3707 mL
100 mM 0.0274 mL 0.1371 mL 0.2741 mL 0.6853 mL

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TargetMol Library Books参考文献

1. Jo H, et al. Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death. Proc Natl Acad Sci U S A. 2012 Jun 26;109(26):10581-6. 2. Gopallawa I, et al. Small-molecule Akt-activation in airway cells induces NO production and reduces IL-8 transcription through Nrf-Respir Res. 2021 Oct 19;22(1):267. 3. Jing ZT, et al. AKT activator SC79 protects hepatocytes from TNF-α-mediated apoptosis and alleviates d-Gal/LPS-induced liver injury. Am J Physiol Gastrointest Liver Physiol. 2019 Mar 1;316(3):G387-G396. 4. Shi W, Tang Y, Zhi Y, et al. Akt inhibition-dependent downregulation of the Wnt/β-Catenin Signaling pathway contributes to antimony-induced neurotoxicity. Science of the Total Environment. 2020, 737: 140252.

TargetMol Library Books文献引用

1. Chen H, He A, Li H, et al. TSSK4 upregulation in alveolar epithelial type-II cells facilitates pulmonary fibrosis through HSP90-AKT signaling restriction and AT-II apoptosis. Cell Death & Disease. 2021, 12(10): 1-1 2. Liu Y, Lv H, Li X, et al. Cyclovirobuxine inhibits the progression of clear cell renal cell carcinoma by suppressing the IGFBP3-AKT/STAT3/MAPK-Snail signalling pathway. International Journal of Biological Sciences. 2021, 17(13): 3522-3537. 3. Zhang H, Xia P, Liu J, et al. ATIC inhibits autophagy in hepatocellular cancer through the AKT/FOXO3 pathway and serves as a prognostic signature for modeling patient survival. International Journal of Biological Sciences. 2021, 17(15): 4442-4458. 4. Xu Y, Jiang E, Shao Z, et al. LncRNA FENDRR in Carcinoma-Associated Fibroblasts Regulates the Angiogenesis of Oral Squamous Cell Carcinoma Through the PI3K/AKT Pathway. Frontiers in Oncology. 2021, 11. 5. Wang X, Zhu P, Xu S, et al. Antimony, a novel nerve poison, triggers neuronal autophagic death via reactive oxygen species-mediated inhibition of the protein kinase B/mammalian target of rapamycin pathway. The International Journal of Biochemistry & Cell Biology. 2019, 114: 105561 6. Shi W, Tang Y, Zhi Y, et al Akt inhibition-dependent downregulation of the Wnt/β-Catenin Signaling pathway contributes to antimony-induced neurotoxicity. Science of the Total Environment. 2020, 737: 140252 7. Chen C, Zhang H, Hou S, et al. Shenxian-Shengmai Oral Liquid Evoke Autophagy of Fibroblast to Attenuate Sinoatrial Node Fibrosis in Sick Sinus Syndrome Mice via the AKT/mTOR Pathway. Evidence-Based Complementary and Alternative Medicine. 2022 8. Wang J, Yu Z, Jiang Y, et al.Downregulation of MTHFD2 Inhibits Proliferation and Enhances Chemosensitivity in Hepatocellular Carcinoma via PI3K/AKT Pathway.Frontiers in Bioscience-Landmark.2024, 29(1): 35. 9. Liu Y, Hou Y, Zhang F, et al.ENO1 deletion potentiates ferroptosis and decreases glycolysis in colorectal cancer cells via AKT/STAT3 signaling.Experimental and Therapeutic Medicine.2024, 27(4): 1-9.
Buddlejasaponin IV Scutellarin Icariside B1 N-​Feruloyloctopamine Combretastatin A-1 CCT128930 Hederacolchiside A1 Phellodendrine

相关化合物库

该产品包含在如下化合物库中:
抗乳腺癌化合物库 氧化还原化合物库 抗抑郁症化合物库 抗胰腺癌化合物库 代谢化合物库 抗前列腺癌化合物库 细胞重编程化合物库 抗结直肠癌化合物库 激酶抑制剂库 血管生成库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

SC79 305834-79-1 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt SC 79 inhibit 2-氨基-6-氯-alpha-氰基-3-(乙氧羰基)-4H-1-苯并吡喃-4-乙酸乙酯 Protein kinase B Inhibitor SC-79 PKB inhibitor

 

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