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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.
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PERK Products |
|---|
| WAY-354896
WAY-354896 is a Dual activator of Protein Kinase R (PKR) and Protein Kinase R-Like Kinase (PERK). |
| CCT020312
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells. |
| trans-ISRIB
trans-ISRIB is a integrated stress response (ISR) inhibitor. |
| Salubrinal
Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM. |
| 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. |
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