货号:A306277
同义名:
GSK2399872A;GSK'872
GSK-872是一种 RIPK3 抑制剂,IC50 为 1.8 nM,激酶活性 IC50 为 1.3 nM。它还表现出抑制由 Toll 样受体 3 引发的坏死。
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描述 | GSK-872 is an inhibitor of RIPK3 that binds to the RIP3 kinase domain with an IC50 of 1.8 nM, and it inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 reduces RIPK3-mediated necroptotic cell death, subsequent cytoplasmic translocation, and expression of HMGB1, improving early brain injury-related cerebral edema and neurological deficits[1][2][3]. Within a concentration range of 0.01-3 μM, GSK-872 blocks TNF-induced necroptotic cell death in human HT-29 cells in a concentration-dependent manner over 24 hours[1]. |
Animal study | Administered intracerebroventricularly at 25 mM, GSK-872 alleviates cerebral edema and improves neurological functions following subarachnoid hemorrhage (SAH), and reduces the number of necrotic cells. GSK-872 also lowers the protein levels of RIPK3 and MLKL, as well as the cytoplasmic translocation and expression of the pro-inflammatory protein HMGB1[3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.04mL 2.61mL 1.30mL |
26.08mL 5.22mL 2.61mL |
CAS号 | 1346546-69-7 |
分子式 | C19H17N3O2S2 |
分子量 | 383.487 |
别名 | GSK2399872A;GSK'872 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Room temperature |
溶解方案 |
DMSO: 105 mg/mL(273.8 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |