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
产品货号 : M13450
cas no: 2162961-71-7
BI-2545 是一种新型有效、选择性、口服 Autotaxin 抑制剂,对人和大鼠 ATX 的 IC50 值分别为 2.1 和 3.4 nM。 -
PAT-505
产品货号 : M12680
cas no: 1782070-85-2
PAT-505 (PAT 505, PAT505) 是一种有效的、选择性的、非竞争性的、口服活性的自分泌运动因子抑制剂,对人 ATX 的 lysoPLD 活性的 IC50 为 2.0 nM。 -
GLPG-1690
产品货号 : M12426
cas no: 1628260-79-6
GLPG-1690(Ziritaxestat,GLPG1690)是一种一流的、有效的、竞争性的自分泌运动因子抑制剂,Ki/IC50 为 15 nM/131 nM。 -
Autotaxin inhibitor compound 1
产品货号 : M12375
cas no: 1619971-30-0
Autotaxin抑制剂化合物1 (Autotaxin-IN-1)是一种有效的、选择性的、口服生物可利用的autotaxin抑制剂,在离体人全血测定中IC50为2.2 nM。 -
Autotaxin inhibitor 12
产品货号 : M12344
cas no: 1613513-14-6
Autotaxin抑制剂12是一种高效、选择性、口服生物可利用的autotaxin抑制剂,在胆碱释放测定中IC50为3.1 nM。