Autotaxin
Autotaxin (ATX) is a recently discovered phospholipase D that transforms lysophosphatidylcholine (lpc) into lysophosphatidic acid (lpa). The protein was described as a motility factor for about 10 years until its catalytic capacity was understood. Autotaxin has been identified as a marker of various types of diseases or pre-disease conditions, and it is expressed in a large number of tissues. ATX seems to play a major role downstream of known oncogenes. It has been shown that ATX is induced by the over-expression and/or activation of some key oncogenes, such as ras, jun, rhoC, myc (lpa regulated c-myc, turning the system into a loop), possibly fyn, and the protooncogene wnt-1 or integrins reported on the pathway(s) activated by ATX expression. Enhanced ATX expression has been repeatedly demonstrated in various tumours, including non-small cell lung cancer, breast cancer, renal cell cancer, hepatocellular carcinoma and thyroid cancer and should be enough to suggest that ATX is a potential chemotherapeutic target.
References
1. Boutin JA,et al. Cell Mol Life Sci. 2009 Sep;66(18):3009-21.
References
1. Boutin JA,et al. Cell Mol Life Sci. 2009 Sep;66(18):3009-21.
Wnt/Notch/Hedgehog
Autotaxin
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BI-2545
catalog no : M13450
cas no: 2162961-71-7
BI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively. -
PAT-505
catalog no : M12680
cas no: 1782070-85-2
PAT-505 (PAT 505, PAT505) is a potent, selective, noncompetitive, and orally active autotaxin inhibitor with IC50 of 2.0 nM against the lysoPLD activity of human ATX. -
GLPG-1690
catalog no : M12426
cas no: 1628260-79-6
GLPG-1690 (Ziritaxestat, GLPG1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM. -
Autotaxin inhibitor compound 1
catalog no : M12375
cas no: 1619971-30-0
Autotaxin inhibitor compound 1 (Autotaxin-IN-1) is a potent, selective, orally bioavailable inhibitor of autotaxin with IC50 of 2.2 nM in ex vivo human whole blood assay. -
Autotaxin inhibitor 12
catalog no : M12344
cas no: 1613513-14-6
Autotaxin inhibitor 12 is a highly potent, selective, orally-bioavailable inhibitor of autotaxin with IC50 of 3.1 nM in choline release assays.