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PF-4708671
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-4708671图片
CAS NO:1255517-76-0
规格:98%
分子量:390.41
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
P70 S6K1 isoform inhibitor,cell-permeable
CAS:1255517-76-0
分子式:C19H21F3N6
分子量:390.41
纯度:98%
存储:Store at -20°C

Background:

PF-4708671 is a cell-permeable and highly specific inhibitor of p70 ribosomal S6 kinase 1 with IC50 value of 160nM [1].


S6K1 is a regulator of various biology processes. The inhibition of S6K1 is regard as a therapeutic for the treatment of cancer and insulin resistance. PF-4708671 is the first reported inhibitor of S6K1. It inhibits the activity of S6K1 in the in vitro assay with Ki value of 20nM. For the isolated S6K1 from HEK293 cell, PF-4708671 shows inhibition with IC50 value of 160nM. The inhibition of S6K1caused by PF-4708671 is much more potent than of other related kinases such as RSK2 and MSK1. Besides that, PF-4708671 prevents S6K1 from phosphorylating its substrates including the ribosomal S6 protein, mTOR and Rictor. In addition, PF-4708671 is found to enhance the phosphorylation of S6K1 at Thr229 and Thr389, results in a subsequent increase of S6K1 activity. Whereas this increased activity is much less than that stimulated by IGF1 [1].


参考文献:
[1] Pearce L, Alton G, Richter D, et al. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem. J, 2010, 431: 245-255.