PF-4708671

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0 Metric Ton	Negotiable

0 Metric Ton

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Min.Order :0 Metric Ton
Purity: >97%

Keywords

PF-4708671 S6 Kinase inhibitor & Autophagy activator 1255517-76-0

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Biological Activity

Description

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.

Targets

p70 S6K1 [1]
(Cell-free assay)

160 nM

In vitro

PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. PF-4708671 does not significantly inhibit the activity of the closely related S6K2 isoform or a number of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKC?, PRK2, ROCK2, RSK1, RSK2 or SGK1) . PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 is also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 does not affect activity of mTORC1. [1]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
BHT-101	Growth Inhibition Assay	IC50=0.82024 μM	SANGER
UACC-893	Growth Inhibition Assay	IC50=5.19886 μM	SANGER
A427	Growth Inhibition Assay	IC50=5.72567 μM	SANGER