LOX-IN-3 dihydrochloride

• CAT Number: I044596
• CAS Number: 2409964-23-2
• Molecular Formula: C13H15Cl2FN2O2S
• Molecular Weight: 353.24
• Purity: ≥95%
• Synonyms: (Z)-3-fluoro-4-quinolin-8-ylsulfonylbut-2-en-1-amine;dihydrochloride
• InChI: InChI=1S/C13H13FN2O2S.2ClH/c14-11(6-7-15)9-19(17,18)12-5-1-3-10-4-2-8-16-13(10)12;;/h1-6,8H,7,9,15H2;2*1H/b11-6-
• InChIKey: YYYHSAUHJBNINZ-LEOXJOGCSA-N
• SMILES: C1=CC2=C(C(=C1)S(=O)(=O)CC(=CCN)F)N=CC=C2.Cl.Cl

LOX-IN-3 dihydrochloride is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 dihydrochloride can be used for fibrosis, cancer and angiogenesis research[1].
LOX-IN-3 dihydrochloride monohydrate (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50 values of <10 μM and <1 μM, respectively[1]. LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2[1]. LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities[1].
LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats[1].
LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model[1].
LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice[1].

Reference

[1]. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1.