COMPOUND 52
COMPOUND 52 Basic information
- Product Name:
- COMPOUND 52
- Synonyms:
-
- NG-52
- 2-(2-HYDROXYETHYLAMINO)-6-(3-CHLORANILINO)-9-ISOPROPYLPURINE
- 2-(2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE
- COMPOUND 52
- 2-(2-Hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine, NG-52
- 2-((6-((3-chlorophenyl)aMino)-9-isopropyl-9H-purin-2-yl)aMino)ethanol
- 2-[[6-[(3-Chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]ethanol
- NG 52 (Compound 52 )
- CAS:
- 212779-48-1
- MF:
- C16H19ClN6O
- MW:
- 346.81
- Product Categories:
-
- Inhibitors
- Mol File:
- Mol File
COMPOUND 52 Chemical Properties
- Boiling point:
- 587.7±60.0 °C(Predicted)
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Sealed in dry,2-8°C
- solubility
- methylene chloride: 50 mg/mL, clear, colorless
- form
- powder
- pka
- 14.54±0.10(Predicted)
- color
- white to off-white
MSDS
- Language:English Provider:SigmaAldrich
COMPOUND 52 Usage And Synthesis
Description
NG 52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p (IC50s = 7 and 2 μM, respectively). It is ineffective against the yeast kinases Kin28p, Srb10, and Cak1p. NG 52 is cell permeable and inhibits the growth of S. cerevisiae (GI50 = 30 μM). It is an analog of purvalanol A , a potent inhibitor of mammalian cyclin-dependent kinases.
Uses
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[1][2].
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: | Female nu/nu mice (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. |
IC 50
cdc2-cyclin B: 0.34 μM (IC50); Pho85p: 2 nM (IC50); Cdc28p: 7 μM (IC50); Phosphoglycerate kinase 1 (PGK1): 2.5 μM (IC50)
References
[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. DOI:10.1126/science.281.5376.533
[2] Wen-Liang Wang, et al. Pharmacologically inhibiting phosphoglycerate kinase 1 for glioma with NG52. Acta Pharmacol Sin. 2020 Jul 31. DOI:10.1038/s41401-020-0465-8
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