Molecular Formula | C15H11F2N3 |
Molar Mass | 271.26 |
Density | 1.366±0.06 g/cm3(Predicted) |
Melting Point | 211 °C |
Boling Point | 419.6±40.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
Appearance | powder |
Color | white to beige |
pKa | 5.75±0.50(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
In vitro study | In BCAP-37 cells, Spautin-1 significantly enhanced cell death in glucose-free medium and induced apoptotic cell morphology. spautin-1 inhibits etoposide-induced autophagic cell death in Bax-Bak DKO cells. Spautin-1 prevents degradation of the Vps34 complex and reduces levels of PtdIns3P by modulating the deubiquitinating activity of USP10 and usp13. In PDGF-treated cells, spautin-1 stabilizes α-smooth muscle cell actin and calmodulin, prevents actin fiber disintegration, reduces extracellular matrix production, and abrogate VSMC hyperproliferation and migration. In CML cells, spautin-1 significantly inhibited IM-induced autophagy by down-regulating Beclin-1 and enhanced IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β. In BHK-21 cells, Spautin-1 will also specifically reduce infectious dengue virus. |
In vivo study | Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory cells. |
Hazard Symbols | Xi - Irritant |
Risk Codes | R22 - Harmful if swallowed R41 - Risk of serious damage to eyes |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S39 - Wear eye / face protection. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.686 ml | 18.432 ml | 36.864 ml |
5 mM | 0.737 ml | 3.686 ml | 7.373 ml |
10 mM | 0.369 ml | 1.843 ml | 3.686 ml |
5 mM | 0.074 ml | 0.369 ml | 0.737 ml |
biological activity | Spautin-1 is a potent and specific autodigagy inhibitor that inhibits the deubiquitination activity of USP10 and usp13, the IC50 was 0.6-0.7 μm. Spautin-1 can increase apoptosis. |
Target | Value |
USP10 (Cell-free assay) | 0.5779 μM |
USP13 (Cell-free assay) | 0.6916 μM |