GSK481 is a highly potent and monoselective Receptor Interacting Protein 1 kinase inhibitor. GSK481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cells. GSK481 has approximately equivalent RIP1 FP potencies against human and cynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP.
In vitro: GSK481(benzoxazepinone) not only showed an increase in biochemical activity but also exhibited excellent translation in the U937 cellular assay with IC50 = 10 nM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, et al. J Med Chem. 2016 Mar 10;59(5):2163-78. PMID: 26854747.
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