NG-52
NG 52
CAS: 212779-48-1
Molecular Formula: C16H19ClN6O
NG-52 - Names and Identifiers
NG-52 - Physico-chemical Properties
| Molecular Formula | C16H19ClN6O |
| Molar Mass | 346.81 |
| Density | 1.42±0.1 g/cm3(Predicted) |
| Boling Point | 587.7±60.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| Appearance | powder |
| Color | white to off-white |
| pKa | 14.54±0.10(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
| In vitro study | 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. |
| In vivo study | 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. |
NG-52 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R40 - Limited evidence of a carcinogenic effect R68 - Possible risk of irreversible effects |
| Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
NG-52 - Preparation solution concentration reference
| 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 |
| 5 mM | 0.058 ml | 0.288 ml | 0.577 ml |
Last Update：2024-01-02 23:10:35
NG-52 - Reference Information
| biological activity | NG-52 is a tri-substituted purine that binds to the ATP-binding region of yeast CDK and inhibits Cdc28p and Pho85p, the IC50 values were 7 μm and 2 μm, respectively. |
| Target | TargetValue Pho85p (Cell-free assay) 2 μm Cdc28p (Cell-free assay) 7 μm |
| Target | Value |
| Pho85p (Cell-free assay) | 2 μM |
| Cdc28p (Cell-free assay) | 7 μM |
| in vitro study | NG 52 (Compound 52) 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. |
| Cell Line: | Glioma U87 and U251 cells Glioma U87 and U251 cells |
| Concentration: | 0 μM, 12.5 μM, 25 μM, 50 μM 0 μM, 12.5 μM, 25 μM, 50 μM |
| Incubation Time: | 6 days 12 hours or 24 hours |
| Result: | Potently inhibited the proliferation of primary glioma cells. Potently inhibited the proliferation of primary glioma cells. Dose-dependently suppressed the growth of glioma xenograft. |
| in vivo studies | NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently. 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. |
| 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 |
Last Update：2024-04-09 21:11:58
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Spot supply
Product Name: NG 52 Visit Supplier Webpage Request for quotationCAS: 212779-48-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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