GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. In LNCaP cells, GSK650394 inhibits the androgen-mediated enhancement of Nedd4-2 phosphorylation and androgen-mediated cell growth.GSK650394 counteracts the Cortisol-induced decrease in neurogenesis, changes in Hedgehog signaling, and GR nuclear translocation. [2] GSK 650394 inhibits replication of influenza virus by impairing the export of influenza vRNPs into the cytoplasm of A549 cells.
Molecular Weight | 382.45 |
Formula | C25H22N2O2 |
CAS Number | 890842-28-1 |
Form | Solid |
Solubility (25°C) | 76 mg/mL in DMSO |
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.
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