GSK-843 is a potent receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. GSK-843 inhibits TNF/Z-VAD-FMK/IAP agonist-induced cell necrosis in human mice (EC50 range <0.12 to 3 μM). GSK-843 (0.3-3 μM; 18 h) suppresses TNF-induced death and virus-induced cell necrosis.
| Molecular Weight | 377.49 |
| Formula | C19H15N5S2 |
| CAS Number | 1601496-05-2 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage | -20°C, sealed |
| 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.
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