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GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice.
Front Immunol. 2023 Mar 15;14:1127552.
Giardia duodenalis-induced G0/G1 intestinal epithelial cell cycle arrest and apoptosis involve activation of endoplasmic reticulum stress in vitro
GSK2606414 purchased from AbMole
| Molecular Weight | 451.44 |
| Formula | C24H20F3N5O |
| CAS Number | 1337531-36-8 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PERK Products |
|---|
| MK-28
MK-28 is a potent and selective PERK activator. |
| PERK-IN-4
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. |
| PERK-IN-6
PERK-IN-6 is a PERK inhibitor with an IC50 of 2.5 nM. |
| ML291
ML291 is a first-in-class, potent chemical probe with an EC50 value of 762 nM that selectively activates the PERK/eIF2a/CHOP (apoptosis) arm of the unfolded protein response (UPR) and induces apoptosis in a variety of solid cancer models for leukemia-related studies. |
| 7DG
7DG (7-Desacetoxy-6,7-dehydrogedunin) is a protein kinase R (PKR) inhibitor. 7DG protects macrophages from lethal toxin-induced pyroptosis. |
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Products are for research use only. Not for human use. We do not sell to patients.
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