公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! 抑制剂描述: 产品名称:NSC87877 产品别名:见爱必信官网 英文别名:NSC87877 靶点:SHP CAS:56932-43-5 纯度:≥98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: NSC87877 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. 溶解性:DMSO : 93 mg/mL (184.7 mM) Water : 92 mg/mL (182.7 mM) 体外研究: 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. 体内研究:NSC-87877 almost completely prevented EAE(experimental autoimmune encephalomyelitis) development by blocking the accumulation of inflammatory cells in the CNS(central nervous system). In an intrarenal mouse model of neuroblastoma, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. 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. 产品信息订购:
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