PF 4708671

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Cat.No. 4032 - PF 4708671 | C19H21F3N6 | CAS No. 1255517-76-0
Description: S6K1 inhibitor
Chemical Name: 2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Reviews
Literature

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.

Compound Libraries

PF 4708671 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 390.41
Formula C19H21F3N6
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1255517-76-0
PubChem ID 51371303
InChI Key FBLPQCAQRNSVHB-UHFFFAOYSA-N
Smiles CCC(C=NC=N2)=C2N1CCN(CC4=NC3=CC(C(F)(F)F)=CC=C3N4)CC1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 19.52 50
ethanol 19.52 50

Preparing Stock Solutions

The following data is based on the product molecular weight 390.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.56 mL 12.81 mL 25.61 mL
5 mM 0.51 mL 2.56 mL 5.12 mL
10 mM 0.26 mL 1.28 mL 2.56 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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.

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

7 Citations for PF 4708671

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

Sinha et al (2017) Loss of ULK1 increases RPS6KB1-NCOR1 repression of NR1H/LXR-mediated Scd1 transcription and augments lipotoxicity in hepatic cells. Autophagy 13 169 PMID: 27846372

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

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

Hullinger et al (2015) Environmental enrichment improves learning and memory and long-term potentiation in young adult rats through a mechanism requiring mGluR5 signaling and sustained activation of p70s6k. Neurobiol Learn Mem 125 126 PMID: 26341144

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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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases