NAZ2329

• CAT Number: I045679
• CAS Number: 2809469-05-2
• Molecular Formula: C21H18F3NO4S3
• Molecular Weight: 501.56
• Purity: ≥95%
• Synonyms: N-(benzenesulfonyl)-3-[[2-ethoxy-5-(trifluoromethyl)phenyl]methylsulfanyl]thiophene-2-carboxamide
• InChI: InChI=1S/C21H18F3NO4S3/c1-2-29-17-9-8-15(21(22,23)24)12-14(17)13-31-18-10-11-30-19(18)20(26)25-32(27,28)16-6-4-3-5-7-16/h3-12H,2,13H2,1H3,(H,25,26)
• InChIKey: AKXBLDKCMACKRY-UHFFFAOYSA-N
• SMILES: CCOC1=C(C=C(C=C1)C(F)(F)F)CSC2=C(SC=C2)C(=O)NS(=O)(=O)C3=CC=CC=C3

NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties[1].
NAZ2329 (0-25 μM; 48 hours) dose-dependently inhibits cell proliferation and migration in all cell lines (rat glioblastoma cells bearing C6 clone and human U251 glioblastoma cells) [1].?
NAZ2329 (25 μM; 0-90 min) obviously promotes the phosphorylation level of paxillin at Tyr-118 site, leading to inhibition for PTPR substrate[1].
NAZ2329 (22.5 mg/kg; intraperitoneal injection; twice per week; 40 days) alone? has a moderate inhibitory effect. However, the combination of Temozolomide and NAZ2329 exerts a significantly increased inhibition of tumor growth compared with the control group, the NAZ2329 monotherapy group and the Temozolomide monotherapy group[1].

Reference

[1]. Akihiro Fujikawa, et al. Targeting PTPRZ inhibits stem cell-like properties and tumorigenicity in glioblastoma cells. Sci Rep. 2017 Jul 17;7(1):5609.
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