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> GSK2593074A [1337531-06-2]

GSK2593074A [1337531-06-2]

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Cat# HY-122909-5mg

Size : 5mg

Brand : MedChemExpress


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

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

View All RIP kinase Isoform Specific Products:

View All Isoforms
RIPK1 RIPK2 RIPK3
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].

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

GSK2593074A Related Antibodies

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].

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.
Molecular Weight

465.57

Formula

C27H23N5OS
CAS No.

1337531-06-2
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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]

  • [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.

Complete Stock Solution Preparation Table

* 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.

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
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GSK2593074A Related Classifications

  • Apoptosis
  • RIP kinase
Help & FAQs

Keywords:

GSK2593074A1337531-06-2GSK'074RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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