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GSK-872 {[allProObj[0].p_purity_real_show]}

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.

GSK-872 化学结构 CAS号:1346546-69-7
GSK-872 化学结构
CAS号:1346546-69-7
GSK-872 3D分子结构
CAS号:1346546-69-7
GSK-872 化学结构 CAS号:1346546-69-7
GSK-872 3D分子结构 CAS号:1346546-69-7
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GSK-872 纯度/质量文件 产品仅供科研

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GSK-872 生物活性

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].

GSK-872 动物研究

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].

GSK-872 参考文献

[1]Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95.

[2]Arora D, et al. Deltamethrin induced RIPK3-mediated caspase-independent non-apoptotic cell death in rat primary hepatocytes. Biochem Biophys Res Commun. 2016 Oct 14;479(2):217-223.

[3]Chen T, et al. Inhibiting of RIPK3 attenuates early brain injury following subarachnoid hemorrhage: Possibly through alleviating necroptosis. Biomed Pharmacother. 2018;107:563-570.

GSK-872 实验方案

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

GSK-872 技术信息

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
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