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PF-4708671P70 S6K1 isoform inhibitor,cell-permeable

PF-4708671

Catalog No. B2228
Size Price Stock Qty
10mg $68.00 In stock
25mg $152.00 In stock
50mg $266.00 In stock
100mg $494.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

PF-4708671

Biological Activity

Description PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 values of 20 nM/160 nM,respectively.
Targets p70 S6K1          
IC50 160 nM (Ki=20 nM)          

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Chemical Properties

Cas No. 1255517-76-0 SDF Download SDF
Chemical Name 2-[[4-(5-ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-6-(trifluoromethyl)-1H-benzimidazole
Canonical SMILES CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F
Formula C19H21F3N6 M.Wt 390.41
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PF-4708671 is a cell-permeable and highly specific inhibitor of p70 ribosomal S6 kinase 1 with IC50 value of 160nM [1].

S6K1 is a regulator of various biology processes. The inhibition of S6K1 is regard as a therapeutic for the treatment of cancer and insulin resistance. PF-4708671 is the first reported inhibitor of S6K1. It inhibits the activity of S6K1 in the in vitro assay with Ki value of 20nM. For the isolated S6K1 from HEK293 cell, PF-4708671 shows inhibition with IC50 value of 160nM. The inhibition of S6K1caused by PF-4708671 is much more potent than of other related kinases such as RSK2 and MSK1. Besides that, PF-4708671 prevents S6K1 from phosphorylating its substrates including the ribosomal S6 protein, mTOR and Rictor. In addition, PF-4708671 is found to enhance the phosphorylation of S6K1 at Thr229 and Thr389, results in a subsequent increase of S6K1 activity. Whereas this increased activity is much less than that stimulated by IGF1 [1].

References:
[1] Pearce L, Alton G, Richter D, et al. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem. J, 2010, 431: 245-255.