MilliporeSigma™ Calbiochem™ Autotaxin Inhibitor II, HA130

Description

• A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC 50 ∽28nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics
• Reported to exhibit low cytotoxicity (TD 50 = 83, 105, and 2056μM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10μM
• Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463μg/kg, i.v.) in vivo , the effect appears short-lived as is the case with S32826 (Cat
• No
• 189510).