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Cat. No. M25432
NAZ2329 Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 501.56
Formula C21H18F3NO4S3
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Clement Agoni, et al. RSC Adv. Allosteric inhibition induces an open WPD-loop: a new avenue towards glioblastoma therapy

[2] Akihiro Fujikawa, et al. J Biol Chem. A head-to-toe dimerization has physiological relevance for ligand-induced inactivation of protein tyrosine receptor type Z

[3] Akihiro Fujikawa, et al. Sci Rep. Targeting PTPRZ inhibits stem cell-like properties and tumorigenicity in glioblastoma cells

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Keywords: NAZ2329 supplier, Phosphatase, inhibitors, activators

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