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NSC-87877 disodium

🥰Excellent
Catalog No. T6911Cas No. 56932-43-5
Alias NSC87877

NSC-87877 disodium (NSC87877) 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 disodium

NSC-87877 disodium

🥰Excellent
Purity: 97.89%
Catalog No. T6911Alias NSC87877Cas No. 56932-43-5
NSC-87877 disodium (NSC87877) 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.
Pack SizePriceAvailabilityQuantity
5 mg$39In Stock
10 mg$56In Stock
25 mg$117In Stock
50 mg$196In Stock
100 mg$292In Stock
200 mg$417In Stock
1 mL x 10 mM (in DMSO)$50In Stock
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Purity:97.89%
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Product Introduction

Bioactivity
Description
NSC-87877 disodium (NSC87877) 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&IC50
SHP2:318 nM, SHP1:355 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[1].
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)[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].
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)
AliasNSC87877
Chemical Properties
Molecular Weight503.42
FormulaC19H13N3O7S2·2Na
Cas No.56932-43-5
Smiles[Na+].[Na+].Oc1c(cc(c2cccnc12)S([O-])(=O)=O)\N=N\c1ccc2cc(ccc2c1)S([O-])(=O)=O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (184.74 mM), Sonication is recommended.
H2O: 92 mg/mL (182.75 mM), Sonication is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM1.9864 mL9.9321 mL19.8641 mL99.3206 mL
5 mM0.3973 mL1.9864 mL3.9728 mL19.8641 mL
10 mM0.1986 mL0.9932 mL1.9864 mL9.9321 mL
20 mM0.0993 mL0.4966 mL0.9932 mL4.9660 mL
50 mM0.0397 mL0.1986 mL0.3973 mL1.9864 mL
100 mM0.0199 mL0.0993 mL0.1986 mL0.9932 mL

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