Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NSC-87877 disodium (NSC87877) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 196 | 现货 | ||
5 mg | ¥ 452 | 现货 | ||
10 mg | ¥ 659 | 现货 | ||
25 mg | ¥ 1,360 | 现货 | ||
50 mg | ¥ 2,260 | 现货 | ||
100 mg | ¥ 3,390 | 现货 | ||
200 mg | ¥ 4,920 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 583 | 现货 |
产品描述 | NSC-87877 disodium (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. |
靶点活性 | SHP2:318 nM, SHP1:355 nM |
体外活性 | 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[1]. |
体内活性 | NSC-87877 almost completely prevented EAE(experimental autoimmune encephalomyelitis) development by blocking the accumulation of inflammatory cells in the CNS(central nervous system)[2]. In an intrarenal mouse model of neuroblastoma, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity[3]. 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[4]. |
细胞实验 | Serum-starved cells are pretreated with NSC-87877 (50 μM,3 h) or dimethyl sulfoxide (solvent) and then stimulated with EGF (100 ng/ml, 5 min) or left untreated. Cells are lysed in ice-cold PTP(protein tyrosine phosphatase) lysis buffer. Shp2 or Shp1 in cell lysate supernatants (0.5 mg/each) is immunoprecipitated with an antibody to Shp2 or an antibody to Shp1 plus protein A-Sepharose for 2 h at 4°C. (Only for Reference) |
别名 | NSC87877 |
分子量 | 503.42 |
分子式 | C19H13N3O7S2·2Na |
CAS No. | 56932-43-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (184.7 mM)
H2O: 92 mg/mL (182.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 1.9864 mL | 9.9321 mL | 19.8641 mL | 49.6603 mL |
5 mM | 0.3973 mL | 1.9864 mL | 3.9728 mL | 9.9321 mL | |
10 mM | 0.1986 mL | 0.9932 mL | 1.9864 mL | 4.966 mL | |
20 mM | 0.0993 mL | 0.4966 mL | 0.9932 mL | 2.483 mL | |
50 mM | 0.0397 mL | 0.1986 mL | 0.3973 mL | 0.9932 mL | |
100 mM | 0.0199 mL | 0.0993 mL | 0.1986 mL | 0.4966 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
NSC-87877 disodium 56932-43-5 Apoptosis Metabolism Phosphatase Neuroblastoma inhibit NSC 87877 Inhibitor NSC 87877 disodium PPAR p53 NSC-87877 HSP27 NSC87877 disodium NSC87877 p38 inhibitor