CS-2489
GSK'872
CAS: 1346546-69-7
Molecular Formula: C19H17N3O2S2
CS-2489 - Names and Identifiers
CS-2489 - Physico-chemical Properties
| 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. |
CS-2489 - Reference Information
| biological activity | GSK' 872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor, which binds to RIP3 kinase region with high affinity (IC50 is 1.8 nM), and IC50 for inhibiting enzyme activity is 1.3 nM. Only weakly cross-reactive. |
| target | TargetValue RIP3K (Cell-free say) 1.3 nM |
| Target | Value |
| RIP3K (Cell-free assay) | 1.3 nM |
| in vitro study | when the concentration is 1 μM, GSK' 872 cannot inhibit more than 300 human protein kinases detected. It does not directly inhibit RIP1 kinase. GSK' 872 concentration-dependently prevented TNF-induced necrotizing apoptosis in HT29 cells. In cell experiments, the IC50 of GSK' 872 is 100-1000 times that of the IC50 in cell-free biochemical test. GSK' 872 can also prevent necrotizing apoptosis of primary human neutrophils isolated from whole blood and inhibit TLR3-or DAI-induced death (TLR3 and DAI are two necrotizing apoptotic pathways independent of RIP1). GSK' 872 can induce caspase activation and then apoptotic cell death. |
| in vivo study | in vivo animal model tests, GSK' 872 treatment can significantly reduce the expression of HIF-1α after ischemic injury. |
Last Update：2024-04-09 21:54:55
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Mobile: 609-228-6898
Featured ProductsSpot supply
Product Name: GSK'872 Visit Supplier Webpage Request for quotationCAS: 1346546-69-7
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Multiple SpecificationsSpot supply
Product Name: GSK'872 Request for quotationCAS: 1346546-69-7
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: GSK'872 Visit Supplier Webpage Request for quotationCAS: 1346546-69-7
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: GSK-872 Visit Supplier Webpage Request for quotationCAS: 1346546-69-7
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
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