189511
Autotaxin Inhibitor II, HA130
ATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid
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EMD Millipore
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25 May 2012
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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).
| Product information | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Molar mass | 463.3 | ||
| Protect from Light | Yes | ||
| Hygrocopic | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C24H19BFNO5S | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Regulatory Review |
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