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.
| Molecular Weight | 416.45 |
| Formula | C23H21FN6O |
| CAS Number | 1337532-29-2 |
| Solubility (25°C) | DMSO 20 mg/mL |
| 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 |
|---|
| 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. |
| AMG PERK 44
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy. |
| WAY-354896
WAY-354896 is a Dual activator of Protein Kinase R (PKR) and Protein Kinase R-Like Kinase (PERK). |
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