1. Metabolic Enzyme/Protease
    Apoptosis
  2. Phosphatase
    Apoptosis
  3. NSC-87877 disodium

NSC-87877 disodium 

目录号: HY-18756A
产品使用指南

NSC-87877 disodium 是一种有效的Shp2Shp1 蛋白质酪氨酸磷酸酶抑制剂,IC50 值分别为0.318 μM 和0.355 μM。NSC-87877还抑制双特异性磷酸酶26 (DUSP26)

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NSC-87877 disodium Chemical Structure

NSC-87877 disodium Chemical Structure

CAS No. : 56932-43-5

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Description

NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively[1]. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26)[2].

IC50 & Target

IC50: 0.318 μM (shp2), 0.355 μM (shp1)[1].

In Vitro

NSC-87877 (0-0.5 μM, 5 days) inhibits DUSP26 function in NB cell lines[3].
NSC-87877 (0-0.5 μM, 5 days) results in increased p53 phosphorylation (Ser37 and Ser46) and activation[3].

Cell Viability Assay[2]

Cell Line: p53 wild-type neuroblastoma (NB) cell lines.
Concentration: 0, 0.25, 0.5 μM.
Incubation Time: 5 days.
Result: Resulted in increased p53 phosphorylation (Ser37 and Ser46) and activation, increased activation of downstream p38 effector proteins (heat shock protein 27 (HSP27) and MAP kinase-activated protein kinase 2 (MAPKAPK2)) and poly ADP ribose polymerase/caspase-3 cleavage.
Inhibited DUSP26 function in NB cell lines.
Resulted in apoptosis in many cell lines at varying IC50 levels of 1.84 μM (IMR32), 6.35 μM (SK-N-SH), 8.69 μM (NB-19), 12.6 μM (SMS-KCN), 15.7 μM (SH-SY5Y), 15.8 μM (JF) and 19.0 μM (CHLA-225), respectively.
In Vivo

NSC-87877 (30 mg/kg, IP once daily for 15 days) possesses excellent anti- neuroblastoma activity[3].

Animal Model: Intrarenal neuroblastoma (NB) tumor mouse model in female nude mice[3].
Dosage: 30 mg/kg.
Administration: IP once daily for 15 days.
Result: Significantly inhibited NB tumor growth.
Molecular Weight

503.42

Formula

C₁₉H₁₁N₃Na₂O₇S₂

CAS No.

56932-43-5

SMILES

O=S(C1=C2C=CC=NC2=C(O)C(/N=N/C3=CC=C4C=C(S(=O)(O[Na])=O)C=CC4=C3)=C1)(O[Na])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

NSC-87877 disodiumPhosphataseApoptosisNeuroblastomap53p38PPARHSP27Inhibitorinhibitorinhibit

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