Thio-ccPA is a stabilized analogue of carbacyclic phosphatidic acid (ccPA). It inhibits the lysoPLD activity of Autotaxin (ATX) and acts as an LPA1/3 receptor antagonist. Thio-ccPA decreases the viability of B16F10, A375, and MeWo melanoma cell lines. Addition of endogenous LPA did not reverse these effects in B16F10 cells. Thio-ccPA decreased the number of pulmonary and non-pulmonary metastases in a B16F10 metastatic melanoma mouse model.
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Featured in Publications
1) Xu, Y., G. Jiang, et al. (2006). “Phosphonothioate and Fluoromethylene Phosphonate Analogues of Cyclic Phosphatidic Acid: Novel Antagonists of Lysophosphatidic Acid Receptors.” Journal of Medicinal Chemistry 49(17): 5309.
2) Altman, M. K., V. Gopal, et al. (2010). “Targeting melanoma growth and viability reveals dualistic functionality of the phosphonothionate analogue of carba cyclic phosphatidic acid.” Mol Cancer 9: 140.
