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。

NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC 50 s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC 50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p.

Solid

cdc2-cyclin B 0.34 μM (IC50) Pho85p 2 nM (

NG 52 (Compound 52) inhibits growth in a drug-sensitized yeast strain ( S. cerevisiae ) with a GI50 of 30 μM. NG 52 is active against cdc2-cyclin B with an IC50 value of 340 nM.
NG 52 dose-dependently inhibits the proliferation of glioma U87 and U251 cell lines with GI50 values of 7.8 μM and 5.2 μM, respectively, meanwhile it potently inhibits the proliferation of primary glioma cells.
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.
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

NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently suppresses the growth of glioma xenograft. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Fem

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 75 mg/mL (216.26 mM; Need ultrasonic)配制储备液