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• 產(chǎn)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

• 靶點： cdc2-cyclin B:0.34 μM (IC50);Pho85p:2 nM (IC50);Cdc28p:7 μM (IC50);Phosphoglycerate kinase 1 (PGK1):2.5 μM (IC50);CDK

• 體外研究：
  NG 52 (Compound 52) 抑制藥物致敏酵母菌株 (S. cerevisiae) 的生長，GI50 為 30 μM。NG 52 對 cdc2-cyclin B 具有活性，IC50 值為 340 nM。 NG 52 劑量依賴性地抑制神經(jīng)膠質(zhì)瘤 U87 的增殖和 U251 細胞株的 GI50 值分別為 7.8 μM 和 5.2 μM，同時有效抑制原代膠質(zhì)瘤細胞的增殖。 NG 52 (12.5-50 μM) 有效抑制 U87 和 U251 細胞中 PDHK1 在 Thr338 位點的磷酸化和 PDH 在 Ser293 位點的磷酸化，導致更多的丙酮酸進入克雷布斯循環(huán)，增加 ATP 和 ROS 的產(chǎn)生。 NG 52通過抑制 PGK1 的活性增強丙酮酸脫氫酶 (PDH) 的活性，從而逆轉(zhuǎn) Warburg 效應(yīng)，將細胞葡萄糖代謝從厭氧模式轉(zhuǎn)變?yōu)橛醒跄Ｊ健? 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.

• 體內(nèi)研究：
  NG 52 (50-150 mg/kg；口服給藥；每天；持續(xù) 13 天) 抑制劑量依賴性地抑制神經(jīng)膠質(zhì)瘤異種移植物的生長。 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.

• 參考文獻：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *