Molecular Formula | C16H11N3O3 |
Molar Mass | 293.28 |
Density | 1.461±0.06 g/cm3(Predicted) |
Melting Point | >330℃ |
Boling Point | 651.5±45.0 °C(Predicted) |
Solubility | DMSO: soluble |
Appearance | powder |
Color | brown |
pKa | 14.18±0.20(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Use | Alsterpaullone (9-Nitropaullone) is a highly effective CDK inhibitor. The IC50 values of CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35 are 35 nM, 15 nM, 200 nM and 40 nM respectively. Alsterpaullone is a competitive GSK-3alpha/GSK-3beta inhibitor of ATP, and the IC50 value of the action is 4 nM. Alsterpaullone has anti-tumor activity and has the potential to be used in the research of neurodegenerative and proliferative diseases. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.41 ml | 17.049 ml | 34.097 ml |
5 mM | 0.682 ml | 3.41 ml | 6.819 ml |
10 mM | 0.341 ml | 1.705 ml | 3.41 ml |
5 mM | 0.068 ml | 0.341 ml | 0.682 ml |
biological activity | alsterpaulone (Alp, 9-nitropaulone, NSC 705701) is a potent inhibitor of CDK, the IC50 values for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35 were 35 nM, 15 nM, 200 nM and 40 nM, respectively. Alsterpaulone is also a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with an IC50 value of 4 nM for both GSK-3α and GSK-3β. Alsterpaulone can induce apoptosis by activating caspase-9. Alsterpaulone has anti-tumor activity and has the potential to treat neurodegenerative and proliferative diseases. |
Target | Value |
caspase-9 () | |
GSK-3α (Cell-free assay) | 4 nM |
GSK-3β (Cell-free assay) | 4 nM |
CDK2/cyclin A (Cell-free assay) | 15 nM |
CDK1/cyclin B (Cell-free assay) | 35 nM |