GSK2593074A (Synonyms: GSK'074)
目录号: PL11034 纯度: ≥98%
CAS No. :1337531-06-2
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中文名称
GSK2593074A
中文别名
化合物 T11484;化合物GSK2593074A
英文名称
GSK2593074A
英文别名
GSK'074;GSK2593074A;BDBM50396531;1-[5-[4-amino-7-(1-methylpyrazol-4-yl)thieno[3,2-c]pyridin-3-yl]-2,3-dihydroindol-1-yl]-2-phenylethanone;7-(1-methyl-1H-pyrazol-4-yl)-3-[1-(phenylacetyl)-2,3-dihydro-1H-indol-5-yl]thieno[3,2-c]pyridin-4-amine;CID 53466951;GSK2593074A (GSK'074;GSK-2593074A);Ethanone, 1-[5-[4-amino-7-(1-methyl-1H-pyrazol-4-yl)thieno[3,2-c]pyridin-3-yl]-2,3-dihydro-1H-indol-1-yl]-2-phenyl-;GSK2593074A,GSK-2593074A
Cas No.
1337531-06-2
分子式
C27H23N5Os
分子量
465.57
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK2593074A (GSK’074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1 和 RIP3。
生物活性
GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.
性状
Solid
IC50 & Target[1][2]
RIP1, RIP3
体外研究(In Vitro)
GSK2593074A (GSK’074; 0.01, 0.1, 1, 10, and 100 nM; 6?hours for MOVAS cells; 3 hours for L929 cells) completely rescues cells from necroptosis under different stimuli in both human and murine cells at IC50~3?nM. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK2593074A inhibits necroptosis with an IC50 of ~3?nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GSK2593074A (GSK’074; 0.93?mg/kg/day; i.p. injection; 14 or 28 days) is administrated to Apoe mice immediately following pump implantation. Compared to the DMSO group, GSK2593074A-treated mice show significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) as well as a reduced abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A significantly decreases the extent of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05) . 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]. Zhou T, et al. Identification of a novel class of RIP1/RIP3 dual inhibitors that impede cell death and inflammation in mouse abdominal aortic aneurysm models. Cell Death Dis. 2019 Mar 6;10(3):226.
溶解度数据
In Vitro: DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic)配制储备液
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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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