PF-4708671

• CAT Number: I001017
• CAS Number: 1255517-76-0
• Molecular Formula: C₁₉H₂₁F₃N₆
• Molecular Weight: 390.41
• Purity: ≥95%
• Target: S6 Kinase
• Solubility: DMSO 30 mg/ml; Water < 1 mg/ml
• Storage: 3 years -20C powder
• IC50: 160 nM [1]
• InChI: InChI=1S/C19H21F3N6/c1-2-13-10-23-12-24-18(13)28-7-5-27(6-8-28)11-17-25-15-4-3-14(19(20,21)22)9-16(15)26-17/h3-4,9-10,12H,2,5-8,11H2,1H3,(H,25,26)
• InChIKey: FBLPQCAQRNSVHB-UHFFFAOYSA-N
• SMILES: CC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F

PF-4708671（Cat No.:I001017） is a potent inhibitor of p70 ribosomal S6 kinase (S6K1 subtype) with a high affinity for its target. It exhibits a Ki/IC50 value of 20nM/160nM in cell-free assays, making it effective in inhibiting S6K1 activity. Importantly, it demonstrates a remarkable selectivity for S6K1 compared to S6K2, with a 400-fold preference. Additionally, PF-4708671 shows even greater selectivity for S6K1 over MSK1, RSK1, and RSK2, making it the first reported S6K1-specific inhibitor and a promising tool for studying S6K1-related signaling pathways.

Reference

1:Leukotriene B₄ Metabolism and p70S6 Kinase 1 Inhibitors: PF-4708671 but Not LY2584702 Inhibits CYP4F3A and the ω-Oxidation of Leukotriene B₄ In Vitro and In Cellulo. Archambault AS, Turcotte C, Martin C, Lefebvre JS, Provost V, Laviolette M, Flamand N.PLoS One. 2017 Jan 9;12(1):e0169804. doi: 10.1371/journal.pone.0169804. eCollection 2017. PMID: 28068410 Free PMC Article2:Protective effects of PF-4708671 against N-methyl-d-aspartic acid-induced retinal damage in rats. Hayashi I, Aoki Y, Ushikubo H, Asano D, Mori A, Sakamoto K, Nakahara T, Ishii K.Fundam Clin Pharmacol. 2016 Dec;30(6):529-536. doi: 10.1111/fcp.12216. Epub 2016 Aug 10. PMID: 27371338 3:The p70S6K Specific Inhibitor PF-4708671 Impedes Non-Small Cell Lung Cancer Growth. Qiu ZX, Sun RF, Mo XM, Li WM.PLoS One. 2016 Jan 15;11(1):e0147185. doi: 10.1371/journal.pone.0147185. eCollection 2016. PMID: 26771549 Free PMC Article4:PF-4708671, a specific inhibitor of p70 ribosomal S6 kinase 1, activates Nrf2 by promoting p62-dependent autophagic degradation of Keap1. Park JS, Kang DH, Lee DH, Bae SH.Biochem Biophys Res Commun. 2015 Oct 23;466(3):499-504. doi: 10.1016/j.bbrc.2015.09.059. Epub 2015 Sep 14. PMID: 26381178 5:PF-4708671 activates AMPK independently of p70S6K1 inhibition. Vainer GW, Saada A, Kania-Almog J, Amartely A, Bar-Tana J, Hertz R.PLoS One. 2014 Sep 9;9(9):e107364. doi: 10.1371/journal.pone.0107364. eCollection 2014. PMID: 25202971 Free PMC Article6:Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Pearce LR, Alton GR, Richter DT, Kath JC, Lingardo L, Chapman J, Hwang C, Alessi DR.Biochem J. 2010 Oct 15;431(2):245-55. doi: 10.1042/BJ20101024. PMID: 20704563