1. Apoptosis
  2. RIP kinase
  3. GSK2593074A

GSK2593074A (Synonyms: GSK'074)

Cat. No.: HY-122909 Purity: 99.88%
Handling Instructions

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

For research use only. We do not sell to patients.

GSK2593074A Chemical Structure

GSK2593074A Chemical Structure

CAS No. : 1337531-06-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1479 mL 10.7395 mL 21.4790 mL
5 mM 0.4296 mL 2.1479 mL 4.2958 mL
10 mM 0.2148 mL 1.0740 mL 2.1479 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GSK2593074AGSK'074RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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GSK2593074A
Cat. No.:
HY-122909
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