| Bioactivity | 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]. | ||||||||||||
| Target | IC50: ~6 nM (KMO) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | GSK180 | ||||||||||||
| CAS | 1799725-26-0 | ||||||||||||
| Formula | C10H7Cl2NO4 | ||||||||||||
| Molar Mass | 276.07 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |