NSC87877

SKU: orb1222021

Description

NSC-87877 is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1/2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability/proliferation.

Key Properties

• CAS Number: 56932-43-5
• MW: 503.42
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₃N₃O₇S₂·2Na
• SMILES: C1=CC2=C(C(=O)/C(=N/NC3=CC4=C(C=C3)C=C(C=C4)S(=O)(=O)[O-])/C=C2S(=O)(=O)[O-])N=C1.[Na+].[Na+]
• Target: SHP-2|SHP-1
• Solubility: In Vitro: DMSO : 125 mg/mL (248.30 mM)

Bioactivity

• In Vivo:
  NSC-87877 (30 mg/kg, IP once daily for 15 days) possesses excellent anti-neuroblastoma activity. 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:
  NSC-87877 (0-0.5 μM, 5 days) inhibits DUSP26 function in NB cell lines. NSC-87877 (0-0.5 μM, 5 days) results in increased p53 phosphorylation (Ser37 and Ser46) and activation. Cell Viability Assay Cell line: p53 wild-type neuroblastoma (NB) cell lines. Concentration: 0, 0.25, 0.5 μM. Incubation time: 5 days. 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

SHP-2|SHP-1