559273
S6K1 Inhibitor, PF-4708671
The S6K1 Inhibitor, PF-4708671 controls the biological activity of S6K1. This small molecule/inhibitor is primarily used for Cancer applications.
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Synonym(s):
S6K1 Inhibitor, PF-4708671, (2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor
Empirical Formula (Hill Notation):
C19H21F3N6
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Quality Level
Assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 50 mg/mL, pale yellow
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki = 20 nM; IC50 = 160 nM) and MSK1 (IC50 = 950 nM) kinase activity, exhibiting little or much reduced potency against 85 other protein and lipid kinases (IC50 = 4.7, 9.2, 65 µM, respectively, against RSK1, RSK2, and S6K2; ≤27% inhibition of the rest at 1 µM). Shown to selectively inhibit IGF1- and PMA-stimulated S6K1 substrates phosphorylation in HEK-293 cells in a dose-dependent manner (up to 10 µM) in vitro and alleviate heart remodeling and functional damage in a MI (myocardial infarction) model in mice in vivo (75/mg/kg/daily i.p.).
A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki = 20 nM; IC50 = 160 nM) and MSK1 (IC50 = 950 nM) kinase activity, exhibiting little or much reduced potency against a panel of 75 other protein kinases (IC50 = 4.7, 9.2, 65 µM, respectively, against RSK1, RSK2, and S6K2; ≤27% inhibition of the rest at 1 µM) and 10 lipid kinases (≤6% inhibition at 10 µM). Inhibits IGF1-induced phosphorylation of cellular S6K1 substrates S6 (Ser235/236 and Ser240/244), mTOR (Ser2448), and Rictor (Thr1135) in serum-starved HEK-293 cultures, but not the phoshorylation of MSK or RSK cellular substrates (CREB Ser133 and GSK3α/β Ser21/ Ser9, respectively) upon PMA stimulation even at concentrations as high as 10 µM. Inhibition of S6K1 activation by rapamycin (Cat. Nos. 553210, 553211, & 553212) or S6K1 activity by PF-4708671 (75/mg/kg/daily i.p.) are both shown to alleviate heart remodeling and functional damage following left coronary artery ligation-induced MI (myocardial infarction) in mice in vivo. Cellular PF-4708671 treatment is also reported to result in increased S6K1 phosphorylation, likely due to a blockage of down-stream negative feedback mechanism.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Di, R., et al. 2012. Biochem. J.441, 199.
Pearce, L.R., et al. 2010. Biochem. J.431, 245.
Pearce, L.R., et al. 2010. Biochem. J.431, 245.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Anna L Fricke et al.
Journal of proteome research, 22(3), 768-789 (2023-02-11)
Phosphorylation-dependent signal transduction plays an important role in regulating the functions and fate of skeletal muscle cells. Central players in the phospho-signaling network are the protein kinases AKT, S6K, and RSK as part of the PI3K-AKT-mTOR-S6K and RAF-MEK-ERK-RSK pathways. However
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