NG 52 是一种有效的，选择性的 ATP 兼容且具有口服活性的Cdc28p和Pho85p激酶抑制剂，IC50分别为 7 μM 和 2 μM。NG 52 还以IC50值为 2.5 μM 来抑制磷酸甘油酸激酶 1 (PGK1) 的活性。NG 52 对酵母激酶 Kin28p，Srb10 和 Cak1p 无活性。
| 生物活性 | NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally activeCdc28pandPho85p kinaseinhibitor withIC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity ofphosphoglycerate kinase 1 (PGK1)with anIC50of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p[1][2]. |
| IC50& Target[1][2] | cdc2-cyclin B 0.34 μM (IC50) | Pho85p 2 nM (IC50) | Cdc28p 7 μM (IC50) | Phosphoglycerate kinase 1 (PGK1) 2.5 μM (IC50) |
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体外研究
(In Vitro) | NG 52 (Compound 52) inhibits growth in a drug-sensitized yeast strain (S. cerevisiae) with a GI50of 30 μM. NG 52 is active against cdc2-cyclin B with an IC50value of 340 nM[1].
NG 52 dose-dependently inhibits the proliferation of glioma U87 and U251 cell lines with GI50values of 7.8 μM and 5.2 μM, respectively, meanwhile it potently inhibits the proliferation of primary glioma cells[2].
NG 52 (12.5-50 μM) effectively inhibits the phosphorylation of PDHK1 at Thr338 site and the phosphorylation of PDH at Ser293 site in U87 and U251 cells, resulting in more pyruvic acid entering the Krebs cycle with increased production of ATP and ROS[2].
NG 52 can reverse the Warburg effect by enhancing the activity of pyruvate dehydrogenase (PDH) through inhibiting the activity of PGK1, and switched cellular glucose metabolism from anaerobic mode to aerobic mode[2].
Cell Proliferation Assay[2] | 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[2] | 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. |
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体内研究
(In Vivo) | NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently suppresses the growth of glioma xenograft[2].
| Animal Model: | Femalenu/numice (5-week-old) injected with glioma cells[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 75 mg/mL(216.26 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8834 mL | 14.4171 mL | 28.8342 mL | | 5 mM | 0.5767 mL | 2.8834 mL | 5.7668 mL | | 10 mM | 0.2883 mL | 1.4417 mL | 2.8834 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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