Home Metabolism phosphatase inhibitor NSC87877

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NSC87877 phosphatase inhibitor

Cat.No.S8182

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.
NSC87877 phosphatase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 503.42

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Quality Control

Batch: S818201 DMSO]100 mg/mL]false]Water]100 mg/mL]false]Ethanol]Insoluble]false Purity: 99.84%
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99.84

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (198.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 503.42 Formula

C19H13N3O7S2.2Na

 Storage (From the date of receipt)
CAS No. 56932-43-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC2=C(C=C(C(=C2N=C1)O)N=NC3=CC4=C(C=C3)C=C(C=C4)S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+]

Mechanism of Action

Targets/IC50/Ki
SHP-2
(Cell-free assay)
318 nM
SHP-1
(Cell-free assay)
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22425446/

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