PKM2/PDK1-IN-1

价格：询价

品牌：MedChemExpress(MCE) 品牌认证

货号：HY-149275

产品详情

PKM2/PDK1-IN-1

CAS No. :

MCE 国际站：PKM2/PDK1-IN-1

产品活性：PKM2/PDK1-IN-1 是一种紫草素硫醚衍生物，是 PKM2/PDK1 的双重抑制剂。 PKM2/PDK1-IN-1抑制NSCLC细胞的增殖，并诱导细胞凋亡 (apoptosis)。 PKM2/PDK1-IN-1 诱导细胞间 ROS 产生，调节凋亡蛋白，参与线粒体和死亡受体通路。

研究领域：Metabolic Enzyme/Protease | PI3K/Akt/mTOR | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Apoptosis

作用靶点：Pyruvate Kinase | PDK-1 | Akt | EGFR | Apoptosis

In Vitro: PKM2/PDK1-IN-1 (compound E5) (0.5-4 μM; 24 h) shows a synergistic anticancer effects with Gefitinib (HY-50895).
PKM2/PDK1-IN-1 (0.5 μM; 24 h) regulates the apoptotic proteins of both mitochondrial and death receptor pathway.
PKM2/PDK1-IN-1 (0.5 μM, 1 μM; 24 h) causes the mitochondria transmembrane potential (ΔΨm) dissipation and intracellular ROS accumulation in lung cancer cells.
PKM2/PDK1-IN-1 (1 μM, 2 μM; 24 h) inhibits PDK1 and enhances the downstream PDH activity in H1975 cells.
PKM2/PDK1-IN-1 inhibits intracellular NADPH concentration and increases ATP production of H1975 cells.

In Vivo: PKM2/PDK1-IN-1 (compound E5) (2.4 mg/kg, 4.8 mg/kg; 6 times in 2 days) suppress the growth of H1975 xenograft tumor in nude mice in vivo with low toxic side effects.