| Name | PF-4708671 |
| Description | PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671(PF4708671) is potent for S6K1(Ki50=20 nM, IC50=160 nM). |
| Kinase Assay | 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. |
| In vivo | PF-4708671 inhibits the phosphorylation of S6 protein mediated by S6K1 in response to IGF-1 (Insulin-like Growth Factor 1) and can also induce the phosphorylation of the T-loop and hydrophobic motif of S6K1 through mTORC1 (mTOR complex 1). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 19.5 mg/mL (49.95 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.12 mM), Sonication is recommended.
Ethanol : 19.5 mg/mL (49.95 mM), Sonication is recommended.
|
| Keywords | S6Kinase | S6K | S6 Kinase | Ribosomal S6 Kinase (RSK) | PF-4708671 | PF 4708671 | p70 S6K | Inhibitor | inhibit | Autophagy |
| Inhibitors Related | Stavudine | Xylitol | Aceglutamide | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Valproic Acid | Curcumin | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | Hematonosis Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
