NSC-87877

• CAT Number: R042372
• CAS Number: 56990-57-9
• Molecular Formula: C₁₉H₁₃N₃O₇S₂
• Molecular Weight: 459.45
• Purity: ≥95%
• Target: Protein Ser/Thr Phosphatases
• Solubility: Soluble in DMSO > 10 mM
• Storage: Store at 4°C
• InChI: InChI=1S/C19H13N3O7S2/c23-19-16(10-17(31(27,28)29)15-2-1-7-20-18(15)19)22-21-13-5-3-12-9-14(30(24,25)26)6-4-11(12)8-13/h1-10,21H,(H,24,25,26)(H,27,28,29)/b22-16+
• InChIKey: BIQBDHSYQMHHPU-CJLVFECKSA-N
• SMILES: C1=CC2=C(C(=O)C(=NNC3=CC4=C(C=C3)C=C(C=C4)S(=O)(=O)O)C=C2S(=O)(=O)O)N=C1

NSC-87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively). NSC-87877 shows effective growth inhibition and induction of apoptosis in NB cell lines. In an intrarenal mouse model of NB, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. DUSP26 inhibition with NSC-87877 is an effective strategy to induce NB cell cytotoxicity in vitro and in vivo through activation of the p53 and p38 mitogen-activated protein kinase (MAPK) tumor-suppressor pathways.

Reference

1:NSC-87877 inhibits DUSP26 function in neuroblastoma resulting in p53-mediated apoptosis. Shi Y, Ma IT, Patel RH, Shang X, Chen Z, Zhao Y, Cheng J, Fan Y, Rojas Y, Barbieri E, Chen Z, Yu Y, Jin J, Kim ES, Shohet JM, Vasudevan SA, Yang J.Cell Death Dis. 2015 Aug 6;6:e1841. doi: 10.1038/cddis.2015.207. PMID: 26247726 Free PMC Article2:NSC-87877, inhibitor of SHP-1/2 PTPs, inhibits dual-specificity phosphatase 26 (DUSP26). Song M, Park JE, Park SG, Lee DH, Choi HK, Park BC, Ryu SE, Kim JH, Cho S.Biochem Biophys Res Commun. 2009 Apr 17;381(4):491-5. doi: 10.1016/j.bbrc.2009.02.069. Epub 2009 Feb 20. PMID: 19233143