NSC-87877

SKU: orb1219514

Description

NSC-87877 is an effective inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (IC50=0.318 μM, 0.355 μM of shp2 and shp1, respectively).It also inhibits dual-specificity phosphatase 26 (DUSP26).

Key Properties

• CAS Number: 56990-57-9
• MW: 459.45
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₃N₃O₇S₂
• SMILES: Oc1c(cc(c2cccnc12)S(O)(=O)=O)\N=N\c1ccc2cc(ccc2c1)S(O)(=O)=O
• Target: Phosphatase
• Solubility: DMSO:4 mg/mL(8.71 mM)

Bioactivity

• In Vivo:
  Animal model: Intrarenal neuroblastoma (NB) tumor mouse model in female nude mice. Dosage: 30 mg/kg. Administration: IP once daily for 15 days. Result: Significantly inhibited NB tumor growth.
• In Vitro:
  Cell Viability Assay Cell line: p53 wild-type neuroblastoma (NB) cell lines. Concentration: 0, 0.25, 0.5 μM. Incubation time: 5 dsys. Result: Resulted in increased p53 phosphorylation (Ser37 and Ser46) and activation, increased activation of downstream p38 effector proteins (heat shock protein 27 (HSP27) and MAP kinase-activated protein kinase 2 (MAPKAPK2)) and poly ADP ribose polymerase/caspase-3 cleavage. Inhibited DUSP26 function in NB cell lines. Resulted in apoptosis in many cell lines at varying IC50 levels of 1.84 μM (IMR32), 6.35 μM (SK-N-SH), 8.69 μM (NB-19), 12.6 μM (SMS-KCN), 15.7 μM (SH-SY5Y), 15.8 μM (JF) and 19.0 μM (CHLA-225), respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Phosphatase