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NSC87877

CAS number:56932-43-5    molecular formula:C19H13N3O7S2.2Na

overview

compound introduction

Information NSC87877 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. Targets SHP-2 (Cell-free assay); SHP-1 (Cell-free assay) 318 nM; 355 nM 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. 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. Cell Research(from reference) Cell lines:HEK293 cells Concentrations:50 μM Incubation Time:3 h

Specs

Chinese alias-
English alias56932-43-5 | NSC87877 | Disodium 8-hydroxy-7-[(6-sulphonato-2-naphthyl)azo]quinoline-5-sulphonate | NSC-87877 disodium | disodium;8-hydroxy-7-[(6-sulfonatonaphthalen-2-yl)diazenyl]quinoline-5-sulfonate | NAPHTHYLAZOXINE S | CHEMBL501993 | 5-Quinolinesulfo
CAS number56932-43-5molecular formulaC19H13N3O7S2.2Na
molecular weight503.42 g/molExact mass10mM in DMSO
PSA189.000 Ųlogp3.899

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