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NAZ2329 is 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. NAZ2329 (25 µM; 0-90 min) obviously promotes the phosphorylation level of paxillin at Tyr-118 site, leading to inhibition for PTPR substrate.
In vivo, NAZ2329 (22.5 mg/kg; intraperitoneal injection; twice per week; 40 days) has a moderate inhibitory effect.
| Molecular Weight | 501.56 |
| Formula | C21H18F3NO4S3 |
| CAS Number | 2809469-05-2 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Phosphatase Products |
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RMC-3943 is an allosteric SHP2 inhibitor (inhibition of full-length SHP2 in biochemical assay, IC50 = 2.19 nM). |
| LYP-IN-1
LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. |
| PF-07284892
PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC50 value of 21 nM. |
| MY10
MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. |
| CPDA
CPDA is a novel potent SH2 domain-containing inositol phosphatase 2 (SHIP2) inhibitor. |
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