GSK-872
目录号: PL11038 纯度: ≥99%
CAS No. :1346546-69-7
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中文名称
GSK-872
中文别名
N-5-苯并噻唑基-6-[(1-甲基乙基)磺酰基]-4-喹啉胺
英文名称
GSK-872
英文别名
GSK'872;GSK872;N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine;N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine;N-(6-(isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine;GSK2399872A;GSK'872 (GSK2399872A);AOB4887;GSK 872;BCP28887;s8465;AK00779012;GSK-872
Cas No.
1346546-69-7
分子式
C19H17N3O2S2
分子量
383.49
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK-872 是 RIPK3 抑制剂,高亲和力结合 RIP3 激酶结构域,IC50为1.8 nM,并抑制激酶活性,IC50为1.3 nM。GSK-872 降低 RIPK3 介导的坏死 (necroptosis) 和随后的 HMGB1 的细胞质易位和表达,并改善早期脑损伤中的脑水肿和神经功能缺损。
生物活性
GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC 50 of 1.8 nM, and inhibits kinase activity with an IC 50 of 1.3 nM. GSK-872 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.
性状
Solid
IC50 & Target[1][2]
IC50: 1.3 nM (RIPK3)
体外研究(In Vitro)
GSK-872 (GSK872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
GSK-872 (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 can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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]. C
溶解度数据
In Vitro: DMSO : 100 mg/mL (260.76 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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