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ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM. ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly.
Patent. CN118161473A 2024 Jun 11.
Patent. CN118161473A
ISRIB purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | AR42j cells |
| Preparation method | The cells were exposed to the ER stress-inducing agent Thapsigargin (Tg, 0.3 μM) in the presence or absence of ISRIB (100 nM) or the PERK kinase inhibitor GSK2606414 (1 μM) for 30 min before lysis. |
| Concentrations | 100 nM |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6J mice |
| Formulation | ISRIB was first reconstituted in dimethyl sulfoxide to the concentration 4 mg/mL and then further diluted using PBS to the final concentration 0.3125 mg/mL. |
| Dosages | 2.5 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 451.34 |
| Formula | C22H24Cl2N2O4 |
| CAS Number | 548470-11-7 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PERK Products |
|---|
| GSK2606414
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. |
| GSK2656157
GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM, 500-fold greater against a panel of 300 kinases. |
| Salubrinal
Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM. |
| trans-ISRIB
trans-ISRIB is a integrated stress response (ISR) inhibitor. |
| CCT020312
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells. |
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