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Spautin-1 是一种自噬抑制剂,可以抑制泛素特异性肽酶 USP10 和 USP13 的去泛素化活性。Spautin-1 抑制 UPR 并在葡萄糖饥饿的癌细胞中显示出优先的细胞毒性。
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Spautin-1 是一种自噬抑制剂,可以抑制泛素特异性肽酶 USP10 和 USP13 的去泛素化活性。Spautin-1 抑制 UPR 并在葡萄糖饥饿的癌细胞中显示出优先的细胞毒性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 457 | 现货 | |
10 mg | ¥ 581 | 现货 | |
50 mg | ¥ 1,995 | 现货 | |
100 mg | ¥ 3,717 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 497 | 现货 |
产品描述 | Spautin-1 is an autophagy inhibitor that suppresses the deubiquitination activity of ubiquitin-specific peptidase USP10 and USP13. Spautin-1 inhibits UPR and exhibits preferential cytotoxicity in glucose-starved cancer cells. |
靶点活性 | K562:1.03 μM |
体外活性 | 方法:A375 和 Sk-Mel-28 细胞用 Spautin-1 (2.5-20 µmol/L) 处理 24-72 h,通过 MTS assay 测定细胞活力。 结果:Spautin-1 以剂量和时间依赖的方式显著降低了 A375 和 SK-Mel-28 的增殖。Spautin-1 对 A375 和 SK-Mel-28 的 72 h IC50 值分别为 1.830 和 2.062 µmol/L。[1] 方法:K562 细胞用 Imatinib mesylate (250 nM) 处理 12 h,再用 Spautin-1 (10 µM) 处理 36 h,通过 Western Blot 检测靶点蛋白表达水平。 结果:Imatinib mesylate 处理后,K562细 胞中的自噬被激活。Spautin-1 对 Imatinib mesylate 诱导的 K562 细胞自噬表现出强烈的抑制作用。[2] |
体内活性 | 方法:为研究对急性胰腺炎的治疗潜力,将 Spautin-1 (2 mg/kg) 腹腔注射给 cerulein 或 L-arginine 诱导胰腺炎的 KunMing 小鼠。 结果:Spautin-1 有效地抑制了自噬通量,改善了由 cerulein 或 L-arginine 诱导的急性胰腺炎的发病机制。Spautin-1 在改善急性胰腺炎中的作用与自噬抑制受损和 Ca2+ 超载缓解有关。[3] 方法:为研究对创伤性脑损伤 (TBI) 后认知和记忆障碍的影响,将 Spautin-1 (10 mmol/uL,2 uL) 注射到左侧脑室。 结果:Spautin-1 给药可能通过激活 caspase-3 来减轻小鼠轻度 TBI 诱导的认知和记忆功能障碍。[4] |
激酶实验 | Kinase inhibitory assays in Vitro: The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802. |
细胞实验 | Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1x105/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi?nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a microplate reader[1]. |
别名 | Spautin 1 |
分子量 | 271.26 |
分子式 | C15H11F2N3 |
CAS No. | 1262888-28-7 |
Smiles | Fc1ccc(CNc2ncnc3ccc(F)cc23)cc1 |
密度 | 1.366 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 45 mg/mL (165.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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