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GSK-481

Chemical Structure : GSK-481

CAS No.: 1622849-58-4

GSK-481 (GSK481;GSK'481)

Catalog No.: PC-42065Not For Human Use, Lab Use Only.

GSK-481 (GSK481) is a highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase (RIPK1) with biochemical IC50 of 10 nM.

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Biological Activity

GSK-481 (GSK481) is a highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase (RIPK1) with biochemical IC50 of 10 nM.
GSK-481 displays complete specificity for RIP1 kinase over a panel of 456 kinases.
GSK-481 exhibits excellent translation in the U937 cellular assay with IC50 of 10 nM, demonstrates significant blockage of the induced RIP1 autophosphorylation at Ser166 in HT29 cells.
GSK-481 possesses good pharmacokinetic profiles in rodents.

Physicochemical Properties

M.Wt 377.3932
Formula C21H19N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 35 mg/mL

Chemical Name/SMILES

3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-

References

1. Harris PA, et al. J Med Chem. 2016 Mar 10;59(5):2163-78.

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