NSC87877 是一种有效的Shp2和Shp1蛋白质酪氨酸磷酸酶抑制剂，IC50值分别为0.318 μM 和0.355 μM。NSC-87877还抑制双特异性磷酸酶26。

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.

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[1].

NSC-87877 almost completely prevented EAE(experimental autoimmune encephalomyelitis) development by blocking the accumulation of inflammatory cells in the CNS(central nervous system)[2]. In an intrarenal mouse model of neuroblastoma, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity[3]. 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[4].

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)

56932-43-5

C19H11N3Na2O7S2

503.41

NSC87877

Ethanol:<1 mgml
DMSO:93 mg/mL (184.7 mM)
H2O:92 mg/mL (182.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years