NSC-87877 disodium 是一种有效的Shp2和Shp1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)。
| 生物活性 | NSC-87877 disodium is a potent inhibitor ofShp2andShp1protein tyrosine phosphatases(SH-PTP2 and SH-PTP1), withIC50values of 0.318 μM, 0.355 μMshp2and shp1, respectively[1]. NSC-87877 also inhibitsdual-specificityphosphatase26 (DUSP26)[2]. |
| IC50& Target | IC50: 0.318 μM (shp2), 0.355 μM (shp1)[1]. |
体外研究
(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 IC50levels 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.
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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