Miltirone

Research use only, not for human use.

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.

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