Autotaxin Inhibitor II, HA130 – Calbiochem

Descrição detalhada : A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 microM 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 10 microM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 microg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826 (Cat. No.189510)., A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 microM 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 10 microM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 microg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826 (Cat. No. 189510).
Sinónimos : Autotaxin Inhibitor II, HA130 - Calbiochem; ATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid
Fórmula molecula r: C24H19BFNO5S
Armazenamento : -20C
Embalagem : 1X10MG