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| Product Name: | GSK872 | | Synonyms: | GSK872;N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine;N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine HCl salt;N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine;CS-2489;GSK-872;GSK 872;GSK872;GSK2399872A;GSK'872;GSK872;GSK2399872A | | CAS: | 1346546-69-7 | | MF: | C19H17N3O2S2 | | MW: | 383.49 | | EINECS: | | Product Categories: | | Mol File: | 1346546-69-7.mol |
| GSK872 Chemical Properties |
| Boiling point | 625.7±55.0 °C(Predicted) | | density | 1.395±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Inert atmosphere,Room temperature | | solubility | Soluble in DMSO (up to at least 25 mg/ml) | | pka | 5.53±0.49(Predicted) | | form | solid | | color | Off-White or pale yellow | | 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. |
| GSK872 Usage And Synthesis |
| Description | GSK 872 (CAS 1346546-69-7) is a potent (IC50 = 1.8nM domain binding; IC50 = 1.3 nM kinase activity) and selective inhibitor of receptor interacting protein 3 (RIP3).1 It is able to prevent necroptosis, virus-induced necrosis, and TLR3-induced necrosis.1,2 GSK872 can induce Caspase8-mediated apoptosis at higher concentrations (e.g.3 μM).2 | | Uses | GSK''872 is a potent and selective receptor activating protein kinase 3 (RIP3) inhibitor (IC50 = 1.3 nM). Exhibits >1000-fold selectivity for RIP3 over a panel of 300 other kinases including RIP1. Inhibits TNF-induced cell death in 3T3-SA cells and TLR3-induced necrosis in fibroblasts in vitro. Blocks necroptosis of primary human neutrophils from whole blood. Also induces apoptosis at higher concentrations (3 - 10 μM). | | Biological Activity | GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity. | | in vitro | When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death. | | in vivo | GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo. | | References | 1)?Kaiser et al. (2013) Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL; J. Biol. Chem.?288 31279
2)?Mandal et al. (2014) RIP3 induces apoptosis independent of pro-necrotic kinase activity; Mol. Cell 56 481 |
| GSK872 Preparation Products And Raw materials |
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