Cat. No.: HY-122909

GSK2593074A

Name: GSK2593074A
Brand: MedChemExpress
SKU: HY-122909
Price: 350.00 USD
Availability: InStock
Rating: 5 (2 reviews)

(Synonyms: GSK'074)

2 Cited Publications

고객리뷰

Based on 2 publication(s) in Google Scholar

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.07%
CAS No.: 1337531-06-2
화학식: C₂₇H₂₃N₅OS
분자량:465.57

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK2593074A Chemical Structure

CAS No.: 1337531-06-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

IC₅₀ & Target

RIP1, RIP3^[1]

All RIP kinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.03 μM Compound: 21	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting	[PMID: 22827572]
L929	IC₅₀	3 nM Compound: GSK2593074A; 18	Anti-necroptic activity in mouse L929 cells incubated for 3 hrs in presence of TNF alpha/zVAD by celltiter-glo assay Anti-necroptic activity in mouse L929 cells incubated for 3 hrs in presence of TNF alpha/zVAD by celltiter-glo assay	[PMID: 36346971]
MOVAS-1	IC₅₀	3 nM Compound: GSK2593074A; 18	Anti-necroptic activity in mouse MOVAS cells incubated for 6 hrs in presence of TNF alpha/zVAD by celltiter-glo assay Anti-necroptic activity in mouse MOVAS cells incubated for 6 hrs in presence of TNF alpha/zVAD by celltiter-glo assay	[PMID: 36346971]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

Cell Viability Assay^[1]

View Protocol

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 1337531-06-2
Appearance Solid
분자량 465.57
화학식 C₂₇H₂₃N₅OS
Color Light yellow to khaki
SMILES

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

GSK'074
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Nat Commun

Mitochondrial vulnerability underlies myocarditis from COVID-19 mRNA vaccine. [Abstract]

2026 Apr 1;17(1):4716. PMID: 41922346
Thromb Haemost

Macrophage ferroptosis promotes MMP2/9 overexpression induced by hemin in hemorrhagic plaque. [Abstract]

2024 Jun;124(6):568-580. PMID: 37696298

용액&용해도

In Vitro:

DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1479 mL	10.7395 mL	21.4790 mL	53.6976 mL
	5 mM	0.4296 mL	2.1479 mL	4.2958 mL	10.7395 mL
	10 mM	0.2148 mL	1.0740 mL	2.1479 mL	5.3698 mL
	15 mM	0.1432 mL	0.7160 mL	1.4319 mL	3.5798 mL
	20 mM	0.1074 mL	0.5370 mL	1.0740 mL	2.6849 mL
	25 mM	0.0859 mL	0.4296 mL	0.8592 mL	2.1479 mL
	30 mM	0.0716 mL	0.3580 mL	0.7160 mL	1.7899 mL
	40 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3424 mL
	50 mM	0.0430 mL	0.2148 mL	0.4296 mL	1.0740 mL
	60 mM	0.0358 mL	0.1790 mL	0.3580 mL	0.8950 mL
	80 mM	0.0268 mL	0.1342 mL	0.2685 mL	0.6712 mL

Bioz

Keywords

GSK2593074A

2 Cited Publications

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GSK2593074A

Publications Citing Use of MedChemExpress (MCE) GSK2593074A

All RIP kinase Isoforms