| 名称 | PF-4708671 |
| 描述 | 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). |
| 激酶实验 | 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. |
| 体内活性 | 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). |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 19.5 mg/mL (50 mM)
Ethanol : 19.5 mg/mL (50 mM)
|
| 关键字 | inhibit | PF-4708671 | S6K | Autophagy | Inhibitor | Ribosomal S6 Kinase (RSK) | PF 4708671 |
| 相关产品 | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相关库 | 糖代谢化合物库 | 经典已知活性库 | 疼痛相关化合物库 | 激酶抑制剂库 | 抑制剂库 | 代谢化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 含氟化合物库 | 抗代谢疾病化合物库 |
United States
