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Chemical Structure : PF-4708671
CAS No.: 1255517-76-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $98 | In stock | |
| 50 mg | $158 | In stock | |
| 100 mg | $258 | In stock | |
| 250 mg | Get quote |
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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.
| M.Wt | 390.414 | |
| Formula | C19H21F3N6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-((4-(5-ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole |
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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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