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Purity: ≥98%
GSK2593074A (also known as GSK’074) is a novel and potent necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3. GSK2593074A showed structural similarities to the well-known RIP3 inhibitor GSK'843. GSK'074 inhibited necroptosis with an IC50 of less than 3 nM in a variety of cell types, including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29). Additionally, GSK'074 but not Nec-1s prevented SMC cytokine production. The biological targets of GSK'074 were determined by biochemical analyses to be RIP1 and RIP3. GSK'074 demonstrated no detectable cytotoxicity even at 20 µM, in contrast to GSK'843, which induces profound apoptosis at high doses (>3 µM).
| Targets |
RIP1; RIP3
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|---|---|
| ln Vitro |
GSK2593074A (GSK'074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) completely prevents necroptosis in both human and murine cells at an IC50 of ~3 nM. GSK2593074A inhibits necroptosis with an IC50 of ~3 nM in a variety of cell types, including mouse SMCs, fibroblasts (L929), bone marrow-derived macrophages (BMDM), and human colon epithelial cells (HT29)[1].
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| ln 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. GSK2593074A-treated mice exhibit significantly lessened aneurysm formation when compared to the DMSO group, as evidenced by a significantly smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) and a decreased incidence of abdominal aortic aneurysm (AAA) (from 83.3 to 16.7%). GSK2593074A significantly reduces the amount of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05)[1].
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| References |
| Molecular Formula |
C27H23N5OS
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|---|---|
| Molecular Weight |
465.569423913956
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| Exact Mass |
465.16233155
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| CAS # |
1337531-06-2
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| Related CAS # |
1337531-06-2
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| Appearance |
Solid
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| SMILES |
CN1C=C(C=N1)C2=CN=C(C3=C2SC=C3C4=CC5=C(C=C4)N(CC5)C(=O)CC6=CC=CC=C6)N
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| InChi Key |
LIGGMBSSOOVGAE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H23N5OS/c1-31-15-20(13-30-31)21-14-29-27(28)25-22(16-34-26(21)25)18-7-8-23-19(12-18)9-10-32(23)24(33)11-17-5-3-2-4-6-17/h2-8,12-16H,9-11H2,1H3,(H2,28,29)
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| Chemical Name |
1-[5-[4-amino-7-(1-methylpyrazol-4-yl)thieno[3,2-c]pyridin-3-yl]-2,3-dihydroindol-1-yl]-2-phenylethanone
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| Synonyms |
GSK2593074A; GSK'074; GSK-2593074A; GSK 074; GSK 2593074A; GSK-074
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 41.7 mg/mL (~89.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Identification of new necroptosis inhibitors.Cell Death Dis.2019 Mar 6;10(3):226. |
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 GSK’074 inhibits necroptosis in various cell types.Cell Death Dis.2019 Mar 6;10(3):226. |
 GSK’074 inhibits aneurysm formation in mouse models of aneurysms.Cell Death Dis.2019 Mar 6;10(3):226. |
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