Autotaxin Inhibitor II, HA130-Calbiochem

半岛bd体育手机客户端 说明

一般描述

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 µM 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 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/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 µM 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 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826 (Cat. No. 189510).

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Albers, H.M.H.G. et al. 2010. J. Med. Chem.53, 4958.
Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA107, 7257.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

半岛bd体育手机客户端 性质

安全信息