Molecular Formula | C19H12Cl2N2O2 |
Molar Mass | 371.22 |
Density | 1.47±0.1 g/cm3(Predicted) |
Melting Point | 287-288.6°C(lit.) |
Boling Point | 598.1±50.0 °C(Predicted) |
Solubility | DMSO: 20mg/mL, soluble |
Appearance | Orange solid |
Color | orange |
pKa | 7.27±0.60(Predicted) |
Storage Condition | -20°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. |
MDL | MFCD09753369 |
Use | SB 216763 |
In vitro study | In addition to inhibiting GSK-3α,SB 216763 is also effective at GSK-3β, inhibiting up to 96% when treated at 10 μm, and has minimal activity when acting on 24 other protein kinases including pkbα and pdk1, IC50>10 μm. SB-216763 acts on human liver cells to stimulate glycogen synthesis with an EC50 of 3.6 μm, and acts on HEK293 cells to induce the transcription of β-catenin-Lef/TCF-related reporter genes in a dose-dependent manner, according to 5 M treatment, the induction reached the maximum value, increased by 2.5 times. Consistent with a significant dose-dependent inhibition of GSK-3 activity, SB 216763 protects cerebellar granule neurons from apoptosis induced by LY-294002 or potassium loss in a concentration-dependent manner, 3 M when the protective nerve reached the highest value, and 10 mM LiCl effect contrast. 3 μm SB 216763 completely inhibited LY-294002-induced death of chicken dorsal root ganglion sensory neurons. 5 μm SB 216763 in HEK293 cells significantly inhibited GSK-3-dependent phosphorylation of neuron-specific microtubule-associated proteins in cerebellar granule neurons and increased the cytoplasmic level of β-catenin, similar to the GSK-3 inhibitory effect of Wnt regulation. 25-50 μm SB 216763 acts on prostate cancer cell lines, including BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC, reducing cell viability in a dose-dependent manner and significantly promoting apoptosis, apoptosis reached 50%, while there was no effect on HMEC or WI38 cell lines. |
In vivo study | SB 216763 treated mice with Bleomycin (BLM)-induced lung inflammation and fibrosis at a dose of 20 mg/kg significantly inhibited the MCP-1 of inflammatory cytokines and the production of TNF-α, lung inflammation and fibrosis were significantly inhibited, and the lifespan of BLM-treated mice was significantly increased. SB 216763 treatment significantly reduced BLM-induced alveoli by inhibiting alveolar epithelial cell injury. |
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 |
HS Code | 29339900 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.694 ml | 13.469 ml | 26.938 ml |
5 mM | 0.539 ml | 2.694 ml | 5.388 ml |
10 mM | 0.269 ml | 1.347 ml | 2.694 ml |
5 mM | 0.054 ml | 0.269 ml | 0.539 ml |