GSK2593074A [1337531-06-2]
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
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:
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. Cell Viability Assay[1]
|
||||||||||||
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.
|
||||||||||||
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 |
|
||||||||||||
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
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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 |
Purity: 98.67% |
||||||||||||
References |
|
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 |
GSK2593074A Related Classifications
- Apoptosis
- RIP kinase