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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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| CCT007093
CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM. |
| Microcystin-LR
Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1. |
| Sal003
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
| Razuprotafib
Razuprotafib (AKB-9778) is an effective selective inhibitor of VE-PTP (HPTPß) catalytic activity (IC50=17 pM). |
| β-Glycerophosphate disodium salt hydrate
β-Glycerophosphate is a classical serine-threonine phosphatase inhibitor used in kinase reaction buffers. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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