NSC87877

Name: NSC87877
Brand: Selleck Chemicals
SKU: S8182
Rating: 5 (4 reviews)

For research use only.

Catalog No.S8182

4 publications

CAS No. 56932-43-5

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.

Selleck's NSC87877 has been cited by 4 publications

Oncotarget, 2020, 21;11(3):265-281

PubMed: 32076487 ( click the link to review the publication )

Cells, 2019, 8(4)

PubMed: 30979083 ( click the link to review the publication )

J Mol Neurosci, 2019, 69(3):360-370

PubMed: 31286407 ( click the link to review the publication )

Front Immunol, 2018, 9:2643

PubMed: 30498494 ( click the link to review the publication )

1 Customer Review

BMDMs and BMDCs were pretreated with NSC87877 (1 μM) for 1 h followed by stimulation with anti-CD180 Ab (0.2 μg/ml). Then the cells were stimulated with R837 (1 μg/ml) and CpG 1826 (0.5 μM). ELISA analysis of the levels of IL-6 and IL-12 secreted by BMDMs (E) and BMDCs (F) at 24 h.

Front Immunol, 2018, 9:2643. NSC87877 purchased from Selleck.

Purity & Quality Control

Choose Selective phosphatase Inhibitors

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

Cell Research:

^[1]

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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.

(Only for Reference)

Animal Research:

^[2]

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Animal Models: C57BL/6 mice
Dosages: 2.5 mg/kg
Administration: i.p.
(Only for Reference)

References

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

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Solubility (25°C)

In vitro	DMSO	100 mg/mL (198.64 mM)
	Water	100 mg/mL (198.64 mM)
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+35% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing.	6mg/mL

* 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.

Chemical Information Download NSC87877 SDF

Molecular Weight	503.42
Formula	C₁₉H₁₃N₃O₇S₂.2Na
CAS No.	56932-43-5
Storage	3 years-20°C powder 2 years-80°C in solvent
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+]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

g

Dosing volume per animal

ul

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Computed Result

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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NSC87877