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GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
| Molecular Weight | 485.29 |
| CAS Number | 2183470-09-7 |
| Solubility (25°C) | DMSO 150 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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