GSK-067
GSK-067 (GSK2593067A) is an inhibitor of necroptosis. GSK-067 inhibits PERK-catalyzed phosphorylation of eIF2α. GSK-067 can be used for research on pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 1337531-05-1
- Formula: C26H21N5OS
- Molecular Weight:451.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| L929 | IC50 |
3 nM
Compound: GSK2593067A; 19
|
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 |
1 nM
Compound: GSK2593067A; 19
|
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
GSK-067 (1-10 μM) is a potent, low-cytotoxicity necroptosis inhibitor in MOVAS and L929 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1337531-05-1
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Molecular Weight 451.55
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Formula C26H21N5OS
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SMILES
O=C(N1C2=CC=C(C=C2CC1)C3=CSC=4C(=CN=C(N)C43)C=5C=NNC5)CC=6C=CC=CC6
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Synonyms
GSK2593067A
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Liu B, et al. WO2023034236A1. PCT/US2022/041936. Published 2023 Mar 9.
[2]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). Journal of medicinal chemistry. 2012 Aug 23;55(16):7193-207. [Content Brief]
[3]. 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 & disease. 2019 Mar 06;10(3):226. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)