NSC87877

Catalog No.S8182 Batch:S8182

Technical Data

Formula	C₁₉H₁₃N₃O₇S₂.2Na
Molecular Weight	503.42	CAS No.	56932-43-5
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (198.64 mM)
		Water	100 mg/mL (198.64 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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 ^[1] (Cell-free assay)	SHP-1 ^[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^[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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HEK293 cells Concentrations 50 μM Incubation Time 3 h Method 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.
Animal Study:^{^[2]}	Animal Models C57BL/6 mice Dosages 2.5 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
HEK293 cells
Concentrations
50 μM
Incubation Time
3 h
Method
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.

Animal Study:^{^[2]}

Animal Models
C57BL/6 mice
Dosages
2.5 mg/kg
Administration
i.p.

References

[4] Peng HY, et al. Pain. 2012, 153(5):1042-53.

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Customer Product Validation

: Data from [Data independently produced by , , Front Immunol, 2018, 9:2643]

Selleck's NSC87877 has been cited by 5 publications

Inhibition of PD-1 Alters the SHP1/2-PI3K/Akt Axis to Decrease M1 Polarization of Alveolar Macrophages in Lung Ischemia-Reperfusion Injury [ Inflammation, 2022, 10.1007/s10753-022-01762-6]	PubMed: 36357527
Resistance to allosteric SHP2 inhibition in FGFR-driven cancers through rapid feedback activation of FGFR. [ Oncotarget, 2020, 21;11(3):265-281]	PubMed: 32076487
Regulation of Microtubule Nucleation in Mouse Bone Marrow-Derived Mast Cells by Protein Tyrosine Phosphatase SHP-1 [ Cells, 2019, 8(4)]	PubMed: 30979083
Nogo-A/Pir-B/TrkB Signaling Pathway Activation Inhibits Neuronal Survival and Axonal Regeneration After Experimental Intracerebral Hemorrhage in Rats. [ J Mol Neurosci, 2019, 69(3):360-370]	PubMed: 31286407
CD180 Ligation Inhibits TLR7- and TLR9-Mediated Activation of Macrophages and Dendritic Cells Through the Lyn-SHP-1/2 Axis in Murine Lupus [Yang Y, et al. Front Immunol, 2018, 9:2643]	PubMed: 30498494

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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