| Molecular Formula | C19H17N3O2S2
|
| Molar Mass | 383.49 |
| Density | 1.395±0.06 g/cm3(Predicted) |
| Boling Point | 625.7±55.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Appearance | Powder |
| Color | Off-White or pale yellow |
| pKa | 5.53±0.49(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| MDL | MFCD30481302 |
| Use | GSK' 872 (GSK2399872A) is a potent, specific RIP3 kinase inhibitor that binds with high affinity to the RIP3 kinase domain (IC50 of 1.8 nM) and inhibits enzyme activity with an IC50 of 1.3 nM. Only with weak cross |
| In vitro study | GSK' 872 was unable to inhibit more than 300 of the human protein kinases tested at a concentration of 1 μm. It does not directly inhibit RIP1 kinase. GSK' 872 concentration-dependently prevented TNF-induced necroptosis of HT29 cells. In the cell assay, the IC50 of GSK's 872 is 100-1000 times that of the cell-free biochemical assay. GSK' 872 also prevents necroptosis of primary human neutrophils isolated from whole blood and inhibits tlr3-or DAI-induced death (TLR3 and DAI are two necroptosis pathways that are independent of RIP1).. GSK' 872 can induce caspase activation followed by apoptotic cell death. |
| In vivo study | In in vivo animal model experiments, treatment with GSK' 872 was able to significantly reduce the expression of HIF-1α after ischemic injury. |
