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GSK2982772 is a potent inhibitor of selective receptor interaction protein kinase 1 (RIPK1), with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively. GSK2982772 binds effectively to RIP1, has sensitive kinase specificity, and has excellent activity in blocking many TNF-dependent cellular responses. RIP1 is an important upstream kinase that has been shown to regulate inflammation through specific functions of scaffold and kinase. In vivo, GSK2982772 showed good free fractions in the blood of rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%).
| Molecular Weight | 377.40 |
| Formula | C20H19N5O3 |
| CAS Number | 1622848-92-3 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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