PS-210 是一种有效的选择性 PDK1 激活剂，Kd 为 3 μM，靶向 PDK1 的 PIF 结合口袋。 PS-210 对其他蛋白激酶无活性，包括 PDK1 下游信号成分，如 S6K、PKB/Akt 或 GS\u200b\u200bK3。在细胞中，PS-210 的前药 (PS423) 作为 PDK1 的底物选择性抑制剂，抑制 S6K 的磷酸化和活化。
货号:ajcx23356
CAS:1221962-86-2
分子式:C19H15F3O5
分子量：380.3
溶解度:DMSO: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PS-210 is an activator of phosphoinositide-dependent protein kinase 1 (PDK1) that increases its thermal stability.^1,2It is selective for PDK-1 over a panel of 120 kinases at 10 µM.¹PS-210 (2 µM) increases the activity of wild-type PDK1 but not PDK1 with a mutation in the PIF-binding pocket.

1.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) 2.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)