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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ribosomal S6 Kinase (RSK)-PF-4708671
PF-4708671

Chemical Structure : PF-4708671

CAS No.: 1255517-76-0

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PF-4708671 (PF4708671)

货号: PC-49024Not For Human Use, Lab Use Only.

PF-4708671 is a potent, specific, cell-permeable inhibitor of S6K1 (p70 ribosomal S6 kinase 1), inhibits the activity of full-length S6K1 in vitro with Ki of 20 nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with IC50 of 160 nM.

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50 mg ￥1580 In stock
100 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-4708671 is a potent, specific, cell-permeable inhibitor of S6K1 (p70 ribosomal S6 kinase 1), inhibits the activity of full-length S6K1 in vitro with Ki of 20 nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with IC50 of 160 nM.
PF-4708671 only inhibited very weakly the closely related S6K2 isoform (IC50=56 μM), as well as RSK1 (IC50=4.7 μM) and RSK2 (IC50=9.2 μM) over 20-fold less potently than S6K1.
PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1, while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases.
PF-4708671 enhances glucose deprivation-induced cell death via downregulation of anti-apoptotic proteins in MCF-7 breast cancer cells.
PF-4708671 inhibits cell migration in a model of metastasis of triple-negative breast cancer.

物理化学性质&存储条件

分子量 390.414
分子式 C19H21F3N6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((4-(5-ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole

参考文献

1. Pearce LR, et al. Biochem J. 2010 Oct 15;431(2):245-55.

2. Rosner M, et al. Amino Acids. 2012 Jun;42(6):2251-6.

3. Parker WE, et al. Sci Transl Med. 2013 Apr 24;5(182):182ra53.

4. Choi HN, et al. Biochem Biophys Res Commun. 2013 Mar 1;432(1):123-8.

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