Original Article:
Monobenzone, a Novel and Potent KDM1A Inhibitor, Suppresses Migration of Gastric Cancer Cells
Peizhi Ma, et al.
Frontiers in Pharmacology, 2021, 12, 640949.
10.3389/fphar.2021.640949
Monobenzone is an organic chemical in the phenol family that is commonly used as a topical drug for medical depigmentation. This study demonstrates that Monobenzone is a novel and potent KDM1A inhibitor that can inhibit the migration of gastric cancer cells.
Lysine-specific demethylase 1 (KDM1A) is often highly expressed in various cancer tissues and is a promising drug target in many cancers. In this study, monobenzone, a topical depigmentation agent clinically used for the treatment of hyperpigmentation, was characterized as a potent inhibitor of KDM1A (IC 50 = 0.4507 μM) with the help of a compound library, which can reversibly competitively inhibit KDM1A. The core highlights of this study include:
> Monobenzone was discovered as a potent and reversible KDM1A inhibitor.
> Monobenzone is a cellular active KDM1A inhibitor.
> Monobenzone inhibits gastric cancer cell migration.
> Monobenzone reverses epithelial mesenchymal transition in gastric cancer cells.
Chemicals Related in the Paper:
| Catalog Number | Product Name | Structure | CAS Number | Price |
|---|---|---|---|---|
| ACM103162 | Monobenzone |  |
103-16-2 | Price |
