| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S84408-1mg买3赠1 |
99.40% | ￥100.00 |
8 | - | - | - | - |
|
S84408-2mg买3赠1 |
99.40% | ￥150.00 |
7 | - | - | - | - |
|
S84408-5mg买3赠1 |
99.40% | ￥200.00 |
8 | - | - | - | - |
|
S84408-10mg |
99.40% | ￥270.00 |
2 | - | - | - | - |
|
S84408-25mg |
99.40% | ￥540.00 |
1 | - | - | - | - |
|
S84408-50mg |
≥99% | ￥1000.00 |
货期：2-3天 | - | - | - | - |
|
S84408-100mg |
≥99% | ￥1800.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p | ||||||||||||||||||||
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| 靶点： | cdc2-cyclin B:0.34 μM (IC50);Pho85p:2 nM (IC50);Cdc28p:7 μM (IC50);Phosphoglycerate kinase 1 (PGK1):2.5 μM (IC50);CDK | ||||||||||||||||||||
| 体外研究： | NG 52 (Compound 52) 抑制药物致敏酵母菌株 (S. cerevisiae) 的生长，GI50 为 30 μM。NG 52 对 cdc2-cyclin B 具有活性，IC50 值为 340 nM。 NG 52 剂量依赖性地抑制神经胶质瘤 U87 的增殖和 U251 细胞株的 GI50 值分别为 7.8 μM 和 5.2 μM，同时有效抑制原代胶质瘤细胞的增殖。 NG 52 (12.5-50 μM) 有效抑制 U87 和 U251 细胞中 PDHK1 在 Thr338 位点的磷酸化和 PDH 在 Ser293 位点的磷酸化，导致更多的丙酮酸进入克雷布斯循环，增加 ATP 和 ROS 的产生。 NG 52通过抑制 PGK1 的活性增强丙酮酸脱氢酶 (PDH) 的活性，从而逆转 Warburg 效应，将细胞葡萄糖代谢从厌氧模式转变为有氧模式。 Cell Proliferation Assay Cell Line: Glioma U87 and U251 cells Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Time: 6 days Result: Potently inhibited the proliferation of primary glioma cells. Western Blot Analysis Cell Line: Glioma U87 and U251 cells Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Time: 12 hours or 24 hours Result: Potently inhibited the proliferation of primary glioma cells. | ||||||||||||||||||||
| 体内研究： | NG 52 (50-150 mg/kg；口服给药；每天；持续 13 天) 抑制剂量依赖性地抑制神经胶质瘤异种移植物的生长。 Animal Model: Female nu/nu mice (5-week-old) injected with glioma cells Dosage: 50 mg/kg, 100 mg/kg, 150 mg/kg Administration: Oral administration; daily; for 13 days Result: Dose-dependently suppressed the growth of glioma xenograft. | ||||||||||||||||||||
| 参考文献： | 1. ray NS, Wodicka L, Thunnissen AM et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8. 2. Wen-Liang Wang, et al. Pharmacologically inhibiting phosphoglycerate kinase 1 for glioma with NG52. Acta Pharmacol Sin. 2020 Jul 31. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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