212779-48-1
212779-48-1 结构式
基本信息
2-[[6-[(3-氯苯基)氨基]-9-异丙基-9H-嘌呤-2-基]氨基]乙醇
2-[[6-[(3-氯苯基)氨基]-9-异丙基-9H-嘌呤-2-基]氨基]乙醇, >98%
NG-52, >98%
COMPOUND 52
NG 52 (Compound 52 )
NG52
COMPOUND52
NG-52
COMPOUND-52
2-(2-HYDROXYETHYLAMINO)-6-(3-CHLORANILINO)-9-ISOPROPYLPURINE
2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]ethanol
2-(2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE
2-((6-((3-chlorophenyl)aMino)-9-isopropyl-9H-purin-2-yl)aMino)ethanol
2-(2-Hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine, NG-52
物理化学性质
常见问题列表
| Target | Value |
|
Pho85p
(Cell-free assay) | 2 μM |
|
Cdc28p
(Cell-free assay) | 7 μM |
NG 52 (Compound 52) inhibits growth in a drug-sensitized yeast strain (
S. cerevisiae
) with a GI
50
of 30 μM. NG 52 is active against cdc2-cyclin B with an IC
50
value of 340 nM.
NG 52 dose-dependently inhibits the proliferation of glioma U87 and U251 cell lines with GI
50
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 to aerobic mode.
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. |
NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently suppresses the growth of glioma xenograft.
| 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. |