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Description: S6K1 inhibitor
Chemical Name: 2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole
Purity: ≥98% (HPLC)
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.12 mL | 25.61 mL | 51.23 mL |
| 2.5 mM | 1.02 mL | 5.12 mL | 10.25 mL |
| 5 mM | 0.51 mL | 2.56 mL | 5.12 mL |
| 25 mM | 0.1 mL | 0.51 mL | 1.02 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
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
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Keywords: PF 4708671, PF 4708671 supplier, PF4708671, selective, inhibitor, inhibitors, p70, ribosomal, S6, kinase, S6K1, inhibits, cancer, Pfizer, RSK, 4032, Tocris Bioscience
9 Citations for PF 4708671
Citations are publications that use Tocris products. Selected citations for PF 4708671 include:
Pirbhoy et al (2017) Synaptically driven phosphorylation of ribosomal protein S6 is differentially regulated at active synapses versus dendrites and cell bodies by MAPK and PI3K/mTOR signaling pathways. Learn Mem 24 341 PMID: 28716954
Melemedjian et al (2013) mTORC1 inhibition induces pain via IRS-1-dependent feedback activation of ERK. Pain 154 1080 PMID: 23607966
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
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
Xing et al (2018) The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development. Front Cell Dev Biol 6 134 PMID: 30364083
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
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
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
Arnold et al (2014) Regulation of cardiac expression of the diabetic marker microRNA miR-29. PLoS One 9 e103284 PMID: 25062042
Do you know of a great paper that uses PF 4708671 from Tocris? Please let us know.
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Literature in this Area
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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