GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasiv e and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA) , and consequently inhibiting ATX-LPA axis -related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 ( IC 50 = 31.42 nM, K i =12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus.
Products | Products > Disease Areas > Cancer | Products > Disease Areas > Melanoma | Products > Disease Areas > Metastatic Melanoma | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Phosphodiesterase (PDE)
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