NSC-87877 disodium

SKU: orb1300353

Description

NSC-87877 is a dual SHP-1 and SHP-2 inhibitor (IC50 ~355 and 318 nM) that suppresses EGF-stimulated Erk1/2 activation in vitro. It demonstrates anti-proliferative effects in breast cancer cell lines and has been utilized in research exploring oncogenic signaling and immune regulation.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 56932-43-5
• MW: 503.42
• Purity: 98.00%
• Formula: C₁₉H₁₃N₃O₇S₂·2Na
• SMILES: [Na+].[Na+].Oc1c(cc(c2cccnc12)S([O-])(=O)=O)\N=N\c1ccc2cc(ccc2c1)S([O-])(=O)=O
• Target: Apoptosis,Phosphatase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:92 mg/mL (182.75 mM);DMSO:93 mg/mL (184.74 mM)

Bioactivity

• Target IC50:
  SHP2:318 nM|SHP1:355 nM
• In Vivo:
  NSC-87877 almost completely prevented EAE(experimental autoimmune encephalomyelitis) development by blocking the accumulation of inflammatory cells in the CNS(central nervous system). In an intrarenal mouse model of neuroblastoma, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. Intrathecal administration of NSC-87877 (an SHP2 antagonist; 1, 10, or 100 μM/rat) into the allodynic rats suppresses spinal nerve ligation-induced allodynia, spinal SHP2 and NR2B phosphorylation, and SHP2/phosphorylated SHP2-PSD-95 and PSD-95-NR2B/phosphorylated NR2B coprecipitation.
• In Vitro:
  NSC-87877 seems to have no selectivity between human Shp2 and Shp1 in vitro. NSC-87877 inhibits EGF-stimulated Shp2 activation and EGF-induced Erk1/2 activation. NSC-87877 suppresses Erk1/2 activation by a Gab1-Shp2 chimera but does not affect PMA(phorbol 12-myristate 13-acetate)-induced Erk1/2 Activation. NSC-87877 does not inhibit EGF-induced Gab1 tyrosine phosphorylation and Gab1-Shp2 association. NSC-87877 can significantly reduce MDA-MB-468 cell viability/proliferation, especially in combination with a phosphoinositide 3-kinase inhibitor.
• Cell Research:
  Serum-starved cells are pretreated with NSC-87877 (50 μM,3 h) or dimethyl sulfoxide (solvent) and then stimulated with EGF (100 ng/ml, 5 min) or left untreated. Cells are lysed in ice-cold PTP(protein tyrosine phosphatase) lysis buffer. Shp2 or Shp1 in cell lysate supernatants (0.5 mg/each) is immunoprecipitated with an antibody to Shp2 or an antibody to Shp1 plus protein A-Sepharose for 2 h at 4°C. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, HSP27, Inhibitor, NSC87877, NSC-87877, NSC87877 disodium, NSC-87877 disodium, Neuroblastoma, p53, inhibit, NSC 87877, NSC 87877 disodium, PPAR, p38, SHP-2, SHP-1, Phosphatase

Compound Identifiers

PubChem CID

92576