货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T98662-1ml促销	10mM in DMSO	￥919.00 ￥826.00 T98662-1ml ￥826.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T98662-1ml促销

10mM in DMSO

￥919.00 ￥826.00

货期：3-5天

产品描述：

磷酸酶抑制剂;phosphatase Inhibitors;;InformationNSC87877 NSC-87877 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.TargetsSHP-2 (Cell-free assay); SHP-1 (Cell-free assay) 318 nM; 355 nMIn vitroNSC-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.In vivoNSC-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.Cell Research(from reference)Cell lines：HEK293 cells Concentrations：50 μM Incubation Time：3 h

靶点：

IC50: 0.318 μM (shp2), 0.355 μM (shp1).

体内研究：

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

参考文献：

1. Chen L, et al. Discovery of a novel shp2 protein tyrosine phosphatase inhibitor. Mol Pharmacol. 2006 Aug;70(2):562-70.
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.
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.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.986 ml	9.932 ml	19.864 ml
5 mM	0.397 ml	1.986 ml	3.973 ml
10 mM	0.199 ml	0.993 ml	1.986 ml
50 mM	0.04 ml	0.199 ml	0.397 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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