Chemical Properties
dark red to red-brown powder
Uses
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].
Biological Activity
Cell permeable: yes', 'Primary Target
SHP1/2 PTPase', 'Product does not compete with ATP.', 'Reversible: no', 'Target IC50: 355 nM and 318 nM against SHP-1 and SHP-2 protein tyrosine phosphatases, respectively
in vivo
NSC-87877 (30mg/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: | 30mg/kg. |
| Administration: | IP once daily for 15 days. |
| Result: | Significantly inhibited NB tumor growth. |
References
[1] Chen L, et al. Discovery of a novel shp2 protein tyrosine phosphatase inhibitor. Mol Pharmacol. 2006 Aug;70(2):562-70. DOI:
10.1124/mol.106.025536[2] Song M, et al. NSC-87877, inhibitor of SHP-1/2 PTPs, inhibits dual-specificity phosphatase 26 (DUSP26). Biochem Biophys Res Commun. 2009 Apr 17;381(4):491-5. DOI:
10.1016/j.bbrc.2009.02.069[3] Y Shi, et al. NSC-87877 inhibits DUSP26 function in neuroblastoma resulting in p53-mediated apoptosis. Cell Death Dis. 2015 Aug 6;6(8):e1841. DOI:
10.1038/cddis.2015.207
