S84408 |
NG 52 |
源叶(MedMol) | 99% |
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- 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
- 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:
1mg 5mg 10mg 1 mM 2.883 ml 14.417 ml 28.834 ml 5 mM 0.577 ml 2.883 ml 5.767 ml 10 mM 0.288 ml 1.442 ml 2.883 ml 50 mM 0.058 ml 0.288 ml 0.577 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)