• 产品描述： GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury

• 靶点： IC50: 1.3 nM (RIPK3);RIPkinase

• 体外研究：
  GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner[1].
  
  They are for reference only.
  
  Cell Viability Assay[1]
  
  Cell Line: HT-29 cells
  Concentration: 0.01, 0.03 , 0.1, 0.3, 1, and 3 μM
  Incubation Time: 24 hours
  Result: Blocked TNF-induced necroptosis in a concentration-dependent manner.

• 体内研究：
  GSK-872 hydrochloride (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 hydrochloride can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein. Animal Model: Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model) Dosage: 25 mM/6 μL Administration: Syringe pump (intracerebroventricular) at 30 min after SAH Result: Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.

• 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.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.381 ml	11.906 ml	23.812 ml
  5 mM	0.476 ml	2.381 ml	4.762 ml
  10 mM	0.238 ml	1.191 ml	2.381 ml
  50 mM	0.048 ml	0.238 ml	0.476 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

• 1. [IF=14] Jiahao Liang et al."Shikonin and chitosan-silver nanoparticles synergize against triple-negative breast cancer through RIPK3-triggered necroptotic immunogenic cell death."BIOMATERIALS".2024 May;:122608

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *