PDK1-IN-RS2 是一种肽对接基序 (PIFtide) 的模拟物,也是一种底物选择性 PDK1 抑制剂,Kd 为 9 μM。PDK1-IN-RS2 抑制 PDK1 对下游激酶 S6K1 的激活。
Cas No. | 1643958-89-7 |
分子式 | C15H9ClN2O2S3 |
分子量 | 380.89 |
溶解度 | DMSO : 125 mg/mL (328.18 mM; Need ultrasonic) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selectivePDK1inhibitor with aKdof 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 byPDK1[1]. PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions[1]. |