PF-4708671 |
| Catalog No.GC10689 |
PF-4708671, is a novel cell-permeable inhibitor of S6K1, specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1255517-76-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
PF-4708671, is a novel cell-permeable inhibitor of S6K1, specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM. [1].
PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), PF-4708671 was also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1) [1]. RSK1, RSK2 and MSK1 were the other kinases inhibited by PF-4708671 (IC50 = 4.7 µM, 9.2 µM and 0.95 µM, respectively). PF-4708671 decreased phosphorylation of ribosomal protein S6 in HEK-293 cells. PF-4708671 has been used as the standard S6K1 inhibitor for the investigation of the role of S6K1 in several cancers. PF-4708671 in combination with tamoxifen was shown to be highly effective against ER+ MCF7 cells that had overexpression of S6K1 [2] and enhanced cell death in glucose-starved MCF7 cells via downregulation of anti-apoptotic proteins Mcl-1 and survivin [3].
PF-4708671 inhibite the AKT/mTOR/S6K1 pathway led to the inhibition of cell migration in triple-negative MDA-MB-231 cells and inhibition of local relapse in mice models [4]. Moreover, PF-4708671 improved glucose tolerance in high-fat -fed obese mice by restoring Akt S473 phosphorylation in metabolic tissues [5]. PF-4708671 has protective effects against NMDA-induced retinal neurotoxicity in rats [6].
References:
[1]. Pearce, L. R. et al. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem. J. 431, 245-255 (2010).
[2]. Hong SE, Kim EK, Jin HO, Kim HA, Lee JK, Koh JS, et al. S6K1 inhibition enhances tamoxifen-induced cell death in MCF-7 cells through translational inhibition of Mcl-1 and survivin. Cell Biol Toxicol. 2013;29(4):273-82.
[3]. Choi HN, Jin HO, Kim JH, Hong SE, Kim HA, Kim EK, et al. Inhibition of S6K1 enhances glucose deprivation-induced cell death via downregulation of anti-apoptotic proteins in MCF-7 breast cancer cells. Biochem Biophys Res Commun. 2013;432(1):123-8.
[4]. Segatto I, Berton S, Sonego M, Massarut S, D'Andrea S, Perin T, et al. Inhibition of breast cancer local relapse by targeting p70S6 kinase activity. J Mol Cell Biol. 2013;5(6):428-31.
[5]. M. Shum, K. Bellmann, P. St-Pierre, A. Marette. Pharmacological inhibition of S6K1 increases glucose metabolism and Akt signalling in vitro and in diet-induced obese mice .Diabetologia, 59 (2016), pp. 592-603
[6]. Hayashi, I.; Aoki, Y.; Ushikubo, H.; Asano, D.; Mori, A.; Sakamoto, K.; Nakahara, T.; Ishii, K. Protective effects of PF-4708671 againstN-methyl-d-aspartic acid-induced retinal damage in rats. Fundam. Clin. Pharmacol. 2016, 30, 529-536.
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *