PF 4708671

Cat. No. 4032

PF 4708671 C19H21F3N6 [1255517-76-0]

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Chemical Name: 2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole

Biological Activity

Cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) (Ki = 20 nM; IC50 = 160 nM). Suppresses the S6K1-mediated phosphorylation of S6, Rictor and mTOR in response to IGF1; displays no effect on the activity of RSK and MSK in vivo. Exhibits no significant inhibition of S6K2 or other AGC kinases (e.g. Akt, PKA and ROCK) in vitro.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
390.41
Formula:
C19H21F3N6
Solubility:
Soluble to 50 mM in DMSO and to 50 mM in ethanol
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1255517-76-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Pearce et al (2010) Characterisation of PF-4708671 a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem.J. 431 245. PMID: 20704563.

If you know of a relevant reference for PF 4708671 please let us know.

Citations are publications that use Tocris products. Selected citations for PF 4708671 include:

Salmond et al (2015) Mechanistic Target of Rapamycin Complex 1/S6 Kinase 1 Signals Influence T Cell Activation Independently of Ribosomal Protein S6 Phosphorylation. J Immunol 195 4615. PMID: 26453749.

Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. Tuberc Respir Dis (Seoul) 5 3145. PMID: 24762669.

Arnold et al (2014) Regulation of cardiac expression of the diabetic marker microRNA miR-29. PLoS One 9 e103284. PMID: 25062042.

Melemedjian et al (2013) mTORC1 inhibition induces pain via IRS-1-dependent feedback activation of ERK. Pain 154 1080. PMID: 23607966.

Wang et al (2011) Convergence of the mammalian target of rapamycin complex 1- and glycogen synthase kinase 3-β-signaling pathways regulates the innate inflammatory response. J Immunol 186 5217. PMID: 21422248.

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Keywords: PF 4708671, supplier, PF4708671, selective, inhibitor, inhibitors, p70, ribosomal, S6, kinase, S6K1, inhibits, cancer, Pfizer, Tocris Bioscience, RSK Inhibitor products

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