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Submit ReviewPF 4708671
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 for PF 4708671
PF 4708671 is a 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 for PF 4708671
PF 4708671 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 4708671
| 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 for PF 4708671
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.52 | 50 | |
| ethanol | 19.52 | 50 |
Preparing Stock Solutions for PF 4708671
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 for PF 4708671
References for PF 4708671
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
If you know of a relevant reference for PF 4708671, please let us know.
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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
18 Citations for PF 4708671
Citations are publications that use Tocris products. Selected citations for PF 4708671 include:
Michelle et al (2017) Autophagy is a signature of a signaling network that maintains hematopoietic stem cells. PLoS One 12 e0177054 PMID: 28486555
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
Min Gyu et al (2022) S6K1 controls adiponectin expression by inducing a transcriptional switch: BMAL1-to-EZH2. Exp Mol Med 54 324-333 PMID: 35338256
Jong Woo et al (2022) Nuclear S6K1 Enhances Oncogenic Wnt Signaling by Inducing Wnt/β-Catenin Transcriptional Complex Formation. Int J Mol Sci 23 PMID: 36555784
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
Markus et al (2023) Selective Eradication of Colon Cancer Cells Harboring PI3K and/or MAPK Pathway Mutations in 3D Culture by Combined PI3K/AKT/mTOR Pathway and MEK Inhibition. Int J Mol Sci 24 PMID: 36675180
Sandra L et al (2023) Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix. iScience 26 105965 PMID: 36824274
George et al (2020) Loss of Kat2a enhances transcriptional noise and depletes acute myeloid leukemia stem-like cells. Elife 9 PMID: 31985402
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
Xing et al (2018) The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development. Front Cell Dev Biol 6 134 PMID: 30364083
Arnold et al (2014) Regulation of cardiac expression of the diabetic marker microRNA miR-29. PLoS One 9 e103284 PMID: 25062042
Lu et al (2021) Cell-type-specific profiling of human cellular models of fragile X syndrome reveal PI3K-dependent defects in translation and neurogenesis. Cell Rep 35 108991 PMID: 33852833
Masao et al (2021) Tofacitinib overcomes an IFNγ-induced decrease in NK cell-mediated cytotoxicity via the regulation of immune-related molecules in LC-2/ad. Thorac Cancer 12 775-782 PMID: 33491334
An-Dao et al (2021) mTORC1 promotes TOP mRNA translation through site-specific phosphorylation of LARP1. Nucleic Acids Res 49 3461-3489 PMID: 33398329
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
Do you know of a great paper that uses PF 4708671 from Tocris? Please let us know.
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