A selective inhibitor of 12-LO (IC50 = 0.34 µM) with greatly reduced potency for 15-LO-1

ML355 – 5 mg

Brand:
Cayman
CAS:
1532593-30-8
Storage:
-20
UN-No:
Non-Hazardous - /

Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.{25127} It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2.{25127} In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.{25127}  

 

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Description

A selective inhibitor of 12-LO (IC50 = 0.34 µM) with greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX1/2; decreases platelet aggregation in patient-derived human platelets and inhibits arachidonic acid and calcium ionophore-induced 12-HpETE in mouse BTC3 cells and human islets

Formal name: N-2-benzothiazolyl-4-[[(2-hydroxy-3-methoxyphenyl)methyl]amino]-benzenesulfonamide

Synonyms: 

Molecular weight: 441.5

CAS: 1532593-30-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Lipoxygenases||Research Area|Immunology & Inflammation||Research Area|Lipid Biochemistry|Lipoxygenase Pathways

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