Molecular Formula | C16H11BrN2O |
Molar Mass | 327.18 |
Melting Point | >300°C (dec.) |
Solubility | DMSO: 18mg/mL, clear, yellow |
Appearance | Yellow-brown solid |
Color | yellow |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
In vitro study | Incubation with prolonged Kenpaullone treatment of HEK-293 cells decreased the level of phosphorylation (Tyr279) of endogenous GSK3α. At the same time, the phosphorylation level of GSK3 beta also decreased. Kenpaullone induced dephosphorylation of GSK3α and GSK3β in SH-SY5Y and PC12 cells; In Escherichia Coli and Sf21 cell lines, Kenpaullone(20 μm) inhibited autophosphorylation of GSK3β(Tyr216). |
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 | 3.056 ml | 15.282 ml | 30.564 ml |
5 mM | 0.611 ml | 3.056 ml | 6.113 ml |
10 mM | 0.306 ml | 1.528 ml | 3.056 ml |
5 mM | 0.061 ml | 0.306 ml | 0.611 ml |
biological activity | kenpaulone (9-bromopaulone, NSC-664704) is an ATP-competitive inhibitor of CDKs, which also inhibits GSK3β, the IC50 was 0.23 μm. |
Target | Value |
GSK-3β (Cell-free assay) | 0.23μM |
CDK1/CyclinB (Cell-free assay) | 0.4μM |
CDK2/CyclinA (Cell-free assay) | 0.68μM |
CDK5/p35 (Cell-free assay) | 0.85μM |
CDK2/CyclinE (Cell-free assay) | 7.5μM |