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PS210 是针对 PDK1的 PIF 结合口袋的、选择性的、有效的 PDK1激活剂,对其他蛋白激酶无活性。在细胞中,它的前药 PS423 可作为 PDK1的底物选择性抑制剂,抑制 S6K 的磷酸化和活化。

PS210 是针对 PDK1的 PIF 结合口袋的、选择性的、有效的 PDK1激活剂,对其他蛋白激酶无活性。在细胞中,它的前药 PS423 可作为 PDK1的底物选择性抑制剂,抑制 S6K 的磷酸化和活化。
| 规格 | 价格 | 库存 | 数量 | 
|---|---|---|---|
| 1 mg | ¥ 276  | In stock | |
| 5 mg | ¥ 618  | In stock | |
| 10 mg | ¥ 987  | In stock | |
| 25 mg | ¥ 1,980  | In stock | |
| 50 mg | ¥ 3,580  | In stock | |
| 100 mg | ¥ 4,950  | In stock | |
| 500 mg | ¥ 9,870  | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 727  | In stock | 
PS210 相关产品
| 产品描述 | PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves as a substrate-selective inhibitor of PDK1 in cells, inhibiting the phosphorylation and activation of S6K.  | 
| 靶点活性 |  PDK1:(kd)3 μM  | 
| 体外活性 | PS210在促使PDK1对温度梯度的稳定中,固定了位于α-B螺旋对侧极端的α-C螺旋另一端的Arg131残基。因此,构成磷酸结合位点的残基似乎是一个固定点,允许在PDK1激活过程中螺旋的相对移动[1]。  | 
| 分子量 | 380.31 | 
| 分子式 | C19H15F3O5 | 
| CAS No. | 1221962-86-2 | 
| Smiles | OC(=O)C(C(CC(=O)c1ccc(cc1)C(F)(F)F)c1ccccc1)C(O)=O | 
| 密度 | 1.400 g/cm3 (Predicted) | 
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 60 mg/mL (157.77 mM), Sonication is recommended.   | |||||||||||||||||||||||||||||||||||
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