Echelon’s fluorogenic Autotaxin (ATX) substrate FS-3 (L-2000) is a doubly labeled analog of LPC wherin the fluorophore is quenched through intramolecular energy transfer. Hydrolysis of the substrate produces an increase in fluorescence.
Autotaxin which has lysophospholipase D (lysoPLD) activity, cleaves choline from lysophosphatidylcholine forming lysophosphatidic acid (LPA), a potent mitogen that as been implicated in the pathophysiology of ovarian cancer. LysoPLD/ATX has been demonstrated to increase cell motility, neovascularization, proliferation, and aggressiveness of tumors and is upregulated in numerous cancer lineages (non-small cell lung , glioma, mammary carcinoma, renal cell carcinoma, hepatocellular carcinoma). In addition, dysregulation of the ATX/LPA pathway is central to the pathophysiology of idiopathic pulmonary fibrosis, rheumatoid arthritis, and other inflammatory diseases. Modulation of ATX activity through small-molecules is a currently underexplored target, but one with high potential for novel cancer and anti-inflammatory therapeutics.
Storage
-20 °C
Solubility
5 mg / mL in H2O or MeOH
Featured in Publications
1) Ferguson, C. G., C. S. Bigman, et al. (2006). “Fluorogenic phospholipid substrate to detect lysophospholipase D/autotaxin activity.” Org Lett 8(10): 2023-6.
2) Baker, D. L., Y. Fujiwara, et al. (2006). “Carba analogs of cyclic phosphatidic acid are selective inhibitors of autotaxin and cancer cell invasion and metastasis.” J Biol Chem 281(32): 22786-93.
3) Parrill, A. L., U. Echols, et al. (2008). “Virtual screening approaches for the identification of non-lipid autotaxin inhibitors.” Bioorg Med Chem 16(4): 1784-95.
4) Hoeglund, A. B., H. E. Bostic, et al. (2010). “Optimization of a pipemidic acid autotaxin inhibitor.” J Med Chem 53(3): 1056-66.
5) Tager, A.M. (2012) “Autotaxin Emerges as a Therapeutic Target for Idiopathic Pulmonary Fibrosis: Limiting Fibrosis by Limiting Lysophosphatidic Acid Synthesis” Am. J. Resp. Cell Mol. Biol. 47(5): 563-565.
Notice to Purchaser: Echelon Biosciences products are sold for research and development purposes only and are not to be incorporated into products for resale without written permission from Echelon Biosciences. The compound FS-3 and its use in assaying for Lysophospholipase D activity are covered by Echelon Biosciences Inc. US patents 7,459,285 & 7,989,663. The purchase of this product includes a limited, non-transferable immunity from suit under the foregoing patent claims for using only this amount of product for the purchaser’s own internal research. For inquiries email busdev@echelon-inc.com
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