NSC87877 - 10mM in DMSO , CAS No.56932-43-5
En stock
SKU
N424808
phosphatase Inhibitors
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
Plus d’information
| CAS | 56932-43-5 |
|---|---|
| Concentration | 10mM in DMSO |
| Synonymes | 56932-43-5|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-Quinolinesulfonic acid, 8-hy |
| Spécifications et pureté | 10mM in DMSO |
| Conditions de stockage de stockage | Store at -80°C |
| Expédié en | Dry ice packs + Cold packs |
| Product Description | 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 |
| PubChem CID | 92576 |
| Formule moléculaire | C19H13N3O7S2.2Na |
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