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GSK 650394

Cat. No. M5325
GSK 650394 Structure
Size Price Availability
5mg USD 90  USD90 Custom Synthesis
10mg USD 140  USD140 Custom Synthesis
50mg USD 480  USD480 Custom Synthesis
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Valinsky WC, et al. J Biol Chem. Aldosterone Upregulates Transient Receptor Potential Melastatin 7 (TRPM7).

[2] Alamares-Sapuay JG, et al. J Virol. Serum- and glucocorticoid-regulated kinase 1 is required for nuclear export of the ribonucleoprotein of influenza A virus.

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  Catalog
Abmole Inhibitor Catalog




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