Miltirone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Miltirone 是一种 CYPs 抑制剂，被定性为中枢苯二氮卓受体的低亲和力配体。 Miltirone 抑制多药耐药 P-糖蛋白 (P-gp) 过表达 CEM/ADR5000 细胞的效果优于药物敏感的 CCRF-CEM 野生细胞。型细胞，这种现象称为附带敏感性。

Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.Miltirone inhibited multidrug-resistant P-glycoprotein (P-gp)-overexpressing CEM/ADR5000 cells better than drug-sensitive CCRF-CEM wild-type cells, a phenomenon termed collateral sensitivity. Flow cytometric analyses revealed that Miltirone induced G2/M arrest and apoptosis. Furthermore, Miltirone stimulated reactive oxygen species (ROS) generation and mitochondrial membrane potential (MMP) disruption, which in turn induced DNA damage and activation of caspases and poly ADP-ribose polymerase (PARP). Downregulation of CCNB1 (cyclin B1) and CDC2 mRNA and upregulation of CDKN1A (p21) mRNA were in accord with Miltirone-induced G2/M arrest. Moreover, Miltirone decreased cell adherence to fibronectin. Molecular docking revealed that Miltirone bound to the ATP-binding site of IKK-β.

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Metabolic Enzyme/Protease

P450

CYP

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27210-57-7

282.38

C19H22O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (177.07 mM)

CC(C)C1=Cc2ccc3c(CCCC3(C)C)c2C(=O)C1=O

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(-20℃)

With Ice Pack

≥ 2 years