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【求助】MAPK通路的抑制剂分种属吗?

丁香园论坛

1629
我想请问各位前辈,我想在大鼠细胞中阻断MAPK通路,请问MAPK通路抑制剂有分种属的吗?除了SIGMA公司的还有哪个公司的比较好啊?谢谢。
那位大侠能回答我这个问题啊,谢谢了!
顶上去
我也要买这个抑制剂,不知道是选择PD98059还是U0126
selleck chemicals 的抑制剂我用过 觉得性价比要比sigma的高很多,而且送货周期也比较短,前些日子还用了他们公司赠送的几个 free sample,还不错 呵呵
德国Merk的不错,我用的SB203580就是Merk的,很不错啊。不过它好像是抑制alpha亚型的


两种的介绍如下:

PD 98059
is a highly selective inhibitor of MEK1 and MEK2 with IC50 values of 4 ?M and 50 ?M respectively. PD98059 does not inhibit activation of other highly related dual-specificity protein kinases or the activity of over 18 other Ser/Thr protein kinases. At concentrations up to 100 ?M, PD98059 does not inhibit activation of MKK3 or SEK (MKK4) as determined by measuring phosphorylation at its activation site.

U0126 is an inhibitor of both MEK1(IC50 of 72 nM) and MEK2(IC50 of 58 nM).
U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways.
The effects of U0126 on the growth of eight human breast cancer cell lines shown that U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types, a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of anchorage entered apoptosis.


更多的细节可以参照 http://www.selleckchem.com/pathways_MEK.html

 

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