计算溶液所需的质量、体积或浓度。
,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
GSK'872 (GSK2399872A)是一种有效的、特异性的RIP3 kinase抑制剂,与RIP3激酶区域以高亲和力结合(IC50为1.8 nM),抑制酶活性的IC50为1.3 nM。仅具微弱交叉反应。
Information
GSK'872 (GSK2399872A) 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.
Cell Data
cell lines:
Concentrations:0.3, 1, 3 μM
Incubation Time:18 h
Powder Purity:≥99%
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。