| Identification | Back Directory | [Name]
N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine | [CAS]
1346546-69-7 | [Synonyms]
GSK872
CS-2489
GSK2399872A
GSK'872 (GSK2399872A)
GSK-872;GSK 872;GSK872
GSK'872;GSK872;GSK2399872A
N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine
N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine
4-Quinolinamine, N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-
N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine HCl salt
N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine HCL SALT // GSK-872 HCL | [Molecular Formula]
C19H17N3O2S2 | [MDL Number]
MFCD30481302 | [MOL File]
1346546-69-7.mol | [Molecular Weight]
383.49 |
| Chemical Properties | Back Directory | [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) | [form ]
solid | [pka]
5.53±0.49(Predicted) | [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. |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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 |
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| Company Name: |
Twochem Co.Ltd
|
| Tel: |
021-58111628 15800915896 |
| Website: |
http://www.twochem.com |
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