Miltirone 是存在于丹参中的一种天然产物，可作为中枢苯二氮受体部分激动剂，IC50值为 0.3 μM。

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[1]

27210-57-7

C19H22O2

282.38

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years