PF4708671 是一种可渗透细胞的 p70 核糖体 S6 激酶抑制剂，对 S6K1的Ki为 20 nM，IC50为 160 nM。

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671 is potent for S6K1(Ki50=20 nM, IC50=160 nM).

PF-4708671可抑制S6K1介导的S6蛋白对IGF-1（胰岛素样生长因子1）的磷酸化反应,还能够通过mTORC1（mTOR复合物1）诱导S6K1的T环和疏水基序的磷酸化。

Affinity determination: Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model.

1255517-76-0

C19H21F3N6

390.414

PF4708671

DMSO:19.5 mg/mL (50 mM)
Ethanol:19.5 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years