货号:A306277 同义名: GSK2399872A;GSK'872
GSK'872 is an inhibitor of RIPK3 with IC50 of 1.8 nM and kinase activity (IC50 = 1.3 nM). It also exhibits supression of necrosis induced by toll-like receptor 3.
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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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
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 |
动物实验配方 |