1. Apoptosis
  2. RIP kinase

GSK2593074A (Synonyms: GSK'074)

目录号: HY-122909
产品使用指南

GSK2593074A (GSK’074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1RIP3

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GSK2593074A Chemical Structure

GSK2593074A Chemical Structure

CAS No. : 1337531-06-2

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Description

GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3[1].

IC50 & Target

RIP1, RIP3[1]

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[1].

Cell Viability Assay[1]

Cell 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 IC50 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) [1].

Animal Model: Apoe-/- female mice (9-10 months)[1]
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.
References
Molecular Weight

465.57

Formula

C₂₇H₂₃N₅OS

CAS No.

1337531-06-2

SMILES

CN1N=CC(C2=CN=C(N)C3=C2SC=C3C4=CC5=C(N(C(CC6=CC=CC=C6)=O)CC5)C=C4)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
GSK2593074A
目录号:
HY-122909
需求量:

GSK2593074A

Cat. No.: HY-122909