PS210
Cat. No.:YN420335
CAS No. :1221962-86-2
产品名称: | PS210 |
CAS No.: | 1221962-86-2 |
Chemical Name: | 2-[3-oxo-1-phenyl-3-[4-(trifluoromethyl)phenyl]propyl]-propanedioic acid |
Synonyms: | PS210 |
分子量: | 380.3146096 |
分子式: | C19H15F3O5 |
SMILES: | FC(F)(F)C1=CC=C(C(CC(C2=CC=CC=C2)C(C(O)=O)C(O)=O)=O)C=C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | PS210 是一种针对PDK1的 PIF 结合口袋的有效且选择性的PDK1激活剂。PS210 对其他蛋白激酶 (包括PDK1下游信号传导成分,如 S6K,PKB/Akt 或 GSK3) 无活性。在细胞中,PS210 的前药 PS423 可作为PDK1的底物选择性抑制剂,抑制 S6K 的磷酸化和活化。 |
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Busschots, K., Lopez-Garcia, L.A., Lammi, C., et al.Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking siteChem. Biol.19(9),1152-1163(2012)
Wilhem, A., Lopez-Garcia, L.A., Busschots, K., et al.2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: Development and prodrug conceptJ. Med. Chem.55(22),9817-9830(2012)