BrP-LPA, aka LPA bromophosphonate, acts as both an Autotaxin inhibitor (94% inhibition at 10 μM) and pan LPA receptor antagonist (LPA1: 1.5 μM, LPA2: 1.4 μM, LPA3: 1.2 μM, LPA4: 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 PPARγ is not activated by BrP-LPA.
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