For research use only. Not for therapeutic Use.
ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
ML355 inhibits PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells[1].
ML355 (1.88-30 mg/kg; i.g.; 2 times per day for two days) strongly inhibits the thrombus formation in mice at higher dose compared to WT controls[3].
| Catalog Number | I001921 |
| CAS Number | 1532593-30-8 |
| Synonyms | N-(1,3-benzothiazol-2-yl)-4-[(2-hydroxy-3-methoxyphenyl)methylamino]benzenesulfonamide |
| Molecular Formula | C21H19N3O4S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H19N3O4S2/c1-28-18-7-4-5-14(20(18)25)13-22-15-9-11-16(12-10-15)30(26,27)24-21-23-17-6-2-3-8-19(17)29-21/h2-12,22,25H,13H2,1H3,(H,23,24) |
| InChIKey | OWHBVKBNNRYMIN-UHFFFAOYSA-N |
| SMILES | COC1=CC=CC(=C1O)CNC2=CC=C(C=C2)S(=O)(=O)NC3=NC4=CC=CC=C4S3 |
| Reference | [1]. Luci DK, et al. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase. J Med Chem. 2014 Jan 23;57(2):495-506. [2]. Zhang XJ, et al. An ALOX12-12-HETE-GPR31 signaling axis is a key mediator of hepatic ischemia-reperfusion injury. Nat Med. 2018 Jan;24(1):73-83. [3]. Adili R, et al. First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis. Arterioscler Thromb Vasc Biol. 2017 Oct;37(10):1828-1839. |
