Description: | BrP-LPA, aka LPA bromophosphonate, acts as both an Autotaxin inhibitor (94% inhibition at 10 µM) and pan LPA receptor antagonist (LPA(1): 1.5 µM, LPA(2): 1.4 µM, LPA(3): 1.2 µM, LPA(4): 0.27 µM). BrP-LPA inhibits the invasiveness of NIH3T3 ras ATX cells by 40% and decreases chemotaxis by 23%. BrP-LPA reduces the size of breast (MDA-MB-231), colon (HCT-116) and melanoma (B16F10) tumors in mouse models. It also attenuates collagen-induced arthritis PPAR" is not activated by BrP-LPA. 1) Jiang, G., Y. Xu, et al. (2007). "Alpha-substituted phosphonate analogues of lysophosphatidic acid (LPA) selectively inhibit production and action of LPA." ChemMedChem 2(5): 679-90. 2) Zhang, H., X. Xu, et al. (2009). "Dual Activity Lysophosphatidic Acid Receptor Pan-Antagonist/Autotaxin Inhibitor Reduces Breast Cancer Cell Migration In vitro and Causes Tumor Regression In vivo." Cancer Res 69: 5441; 3) Schleicher, S. M., D. K. Thotala, et al. (2011). "Autotaxin and LPA Receptors Represent Potential Molecular Targets for the Radiosensitization of Murine Glioma through Effects on Tumor Vasculature." PLoS ONE 6(7): e22182. 4) Nikitopoulou, I., E. Kaffe, et al. (2013). "A Metabolically-Stabilized Phosphonate Analog of Lysophosphatidic Acid Attenuates Collagen-Induced Arthritis." PLoS ONE 8(7): e70941; |
Order #: | ECH-L-7416-5MG |
Unit Size: | 5 mg |
Supplier: | Echelon Biosciences |
Restrictions: | Available in all European countries, except France & Italy. |
Shipping: | Gel Ice |
Storage: | -20 °C or below |
Subcategory: | Biochemical Reagents |
More information: | Go to webpage |
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