JX 06 是一种有效的、选择性的、共价的 PDK 抑制剂。 JX 06 抑制 PDK1、PDK2 和 PDK3，IC50 分别为 49 nM、101 nM 和 313 nM。 JX 06 通过以不可逆方式共价结合半胱氨酸残基来抑制 PDK1 活性。 JX 06 显示出显着的抗肿瘤活性。
| Cas No. | 729-46-4 |
| Canonical SMILES | S=C(SSC(N1CCOCC1)=S)N2CCOCC2 |
| 分子式 | C10H16N2O2S4 |
| 分子量 | 324.51 |
| 溶解度 | Soluble in DMSO |
| 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 | Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor (IC50 values are 49, 101 and 313 nM for PDK1, PDK2 and PDK3, respectively). Exhibits selectivity for PDK1/2/3 over PDK4 and a panel of 323 other kinases. Suppresses A549 lung cancer cell proliferation in vitro. Reduces tumor volume of A549 xenografts in mice. Sun et al (2015) JX06 selectively inhibits pyruvate dehydrogenase kinase PDK1 by a covalent cysteine modification. Cancer Res. 75 4923 PMID:26483203 |
