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GSK2593074A

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 1337531-06-2
  • 分子式: C27H23N5OS
  • 分子量: 465.57
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货号 (SKU) 包装规格 是否现货 价格 数量
G656850-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 GSK2593074A
生化机理 GSK2593074A (GSK'074)是一种坏死抑制剂,对 RIP1 和 RIP3 具有双重靶向能力。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3

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 IC 50 ~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 IC 50 of ~3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929 Concentration: 0.01, 0.1, 1, 10, and 100 nM Incubation Time: 6 hours for MOVAS cells; 3 hours for L929 cells Result: Inhibited MOVAS and L929 cells with the IC 50 of 3 nM.

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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Apoe -/- female mice (9-10 months) Dosage: 0.93 mg/kg/day; 200 µL Administration: Daily i.p. injection; 14 or 28 days Result: Inhibited aneurysm formation in mouse models of aneurysms.

IC50& Target:RIP1, RIP3

关联靶点(人)

EIF2AK3 Tchem 真核翻译起始因子 2-α激酶 3(Eukaryotic translation initiation factor 2-alpha kinase 3) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES CN1C=C(C=N1)C2=CN=C(C3=C2SC=C3C4=CC5=C(C=C4)N(CC5)C(=O)CC6=CC=CC=C6)N
PubChem CID 53466951
分子量 465.57

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