189511
Autotaxin Inhibitor II, HA130
Synonym(s):
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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About This Item
Empirical Formula (Hill Notation):
C24H19BFNO5S
Molecular Weight:
463.29
NACRES:
NA.77
UNSPSC Code:
51111800
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
assay
≥97% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
off-white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
General 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 (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).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
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.
Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA107, 7257.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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