1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. NAZ2329

NAZ2329 

Cat. No.: HY-103693
Handling Instructions

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.

For research use only. We do not sell to patients.

NAZ2329 Chemical Structure

NAZ2329 Chemical Structure

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Description

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].

IC50 & Target

IC50: 7.5 µM (PTPRZ), 4.8 µM (PTPRG), 35.7 µM (PTPRA), 56.7 µM (PTPRM), 23.7 µM (PTPRS), 35.4 µM (PTPRB), 15.2 µM (PTPN6), 14.5 µM (PTPN1)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Rat glioblastoma cells bearing C6 clone, human U251 glioblastoma cells
Concentration: 0 µM, 6.3 µM, 12.5 µM, 25 µM
Incubation Time: 48 hours
Result: Exerted inhibition in cell proliferation and migration in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Rat glioblastoma cells bearing C6 clone
Concentration: 25 µM
Incubation Time: 0 min, 15 min, 30 min, 60 min, 90min
Result: Promoted the phosphorylation level of paxillin at Tyr-118 site.
In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c- nu/nu mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells[1]
Dosage: 22.5 mg/kg; Temozolomide (TMZ, 50 mg/kg)
Administration: Intraperitoneal injection; twice per week; 40 days
Result: The combination of NAZ2329 and TMZ significantly delayed tumor growth compared to NAZ2329 or TMZ alone.
Molecular Weight

501.56

Formula

C₂₁H₁₈F₃NO₄S₃

SMILES

CCOC1=C(CSC2=C(C(NS(=O)(C3=CC=CC=C3)=O)=O)SC=C2)C=C(C(F)(F)F)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

NAZ2329NAZ 2329NAZ-2329PhosphataseallostericantitumorInhibitorinhibitorinhibit

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NAZ2329
Cat. No.:
HY-103693
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