GSK180

Names

[ Name ]:
GSK180

[Synonym ]:
GSK180

Biological Activity

[Description]:

GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

[Target]

IC50: ~6 nM (KMO)[1]

[In Vitro]

GSK180 inhibits endogenous KMO activity in primary human hepatocytes (IC50=2.6 µM). GSK180 inhibits rat KMO slightly less potently than the human enzyme (IC50=7 µM)[1].

[In Vivo]

GSK180 is proper for i.v. administration[1].

[References]

[1]. Mole DJ, et al. Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis. Nat Med. 2016 Feb;22(2):202-9.

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds

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