NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ ( IC 50 =7.5 µM for hPTPRZ1) and PTPRG ( IC 50 =4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment ( IC 50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment ( IC 50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
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