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NSC-87877 disodium

Catalog No. T6911   CAS 56932-43-5
Synonyms: 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
NSC-87877 disodium Chemical Structure
NSC-87877 disodium, CAS 56932-43-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 65.00
10 mg In stock $ 94.00
25 mg In stock $ 195.00
50 mg In stock $ 326.00
100 mg In stock $ 486.00
200 mg In stock $ 695.00
1 mL * 10 mM (in DMSO) In stock $ 83.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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)
Synonyms NSC87877
Molecular Weight 503.42
Formula C19H13N3O7S2·2Na
CAS No. 56932-43-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (184.7 mM)

H2O: 92 mg/mL (182.7 mM)

TargetMolReferences and Literature

1. Chen L, et al. Mol Pharmacol. 2006, 70(2):562-70. 2. Luo Q, et al. Br J Pharmacol. 2014, 171(7):1706-21. 3. Shi Y, et al. Cell Death Dis. 2015, 6:e1841. 4. Peng HY, et al. Pain. 2012, 153(5):1042-53.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Phosphatase Inhibitor Library Lipid Metabolism Compound Library Apoptosis Compound Library Metabolism Compound Library Bioactive Compounds Library Max Bioactive Compound Library Immunology/Inflammation Compound Library Glycometabolism Compound Library

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Keywords

NSC-87877 disodium 56932-43-5 Apoptosis Metabolism Phosphatase Neuroblastoma inhibit NSC 87877 Inhibitor NSC 87877 disodium PPAR p53 NSC-87877 HSP27 NSC87877 disodium NSC87877 p38 inhibitor

 

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