For research use only. Not for therapeutic Use.
Novel type of LTA4H inhibitor (IC50 value of ~0.5 μM in human neutrophils, and Ki value of 2.3 μM for purified LTA4H) that selectively blocks the conversion of LTA4 into proinflammatory mediator LTB4, although leaving the aminopeptidase activity intact for cleavage and inactivation of Pro-Gly-Pro. About LTA4H: Leukotriene A4 hydrolase/aminopeptidase (LTA4H) is a bifunctional zinc metalloenzyme that catalyzes biosynthesis of the proinflammatory mediator, LTB4, implicated in chronic inflammatory diseases. Recently, the chemotactic tripeptide Pro-Gly-Pro was identified as the enzyme’s endogenous peptidase substrate.
KEYWORDS: ARM1 hydrobromide | supplier | LTA4H inhibitor | ARM1 HBr | CAS [1049743-03-4] | [68729-05-5] | Eicosanoid epoxides | LTA4H | Inhibitor | neutrophils | LTA4 | proinflammatory mediator | LTB4 | aminopeptidasePro-Gly-Pro | inflammation
| Catalog Number | R037384 |
| CAS Number | 1049743-03-4 |
| Molecular Formula | C16H14N2S.HBr |
| Purity | ≥95% |
| IUPAC Name | 4-(4-benzylphenyl)-1,3-thiazol-2-amine;hydrobromide |
| InChI | InChI=1S/C16H14N2S.BrH/c17-16-18-15(11-19-16)14-8-6-13(7-9-14)10-12-4-2-1-3-5-12;/h1-9,11H,10H2,(H2,17,18);1H |
| SMILES | C1=CC=C(C=C1)CC2=CC=C(C=C2)C3=CSC(=N3)N.Br |
| Reference | A. Stsiapanava et al. Binding of Pro-Gly-Pro at the active site of leukotriene A4 hydrolase/aminopeptidase and development of an epoxide hydrolase selective inhibitor. Proc. Natl. Acad. Sci. USA. 2014, 111, 4227-4232. |
