RL90

RL90 is a synthetic small molecule cyclohexanone derivative, chemically identified as 2,6-bis(pyridin-3-ylmethylene)-cyclohexanone, that functions as a catalytic inhibitor of DNA topoisomerase I. Unlike traditional topoisomerase I poisons such as camptothecin, which stabilize the covalent enzyme-DNA cleavage complex and lead to double-strand breaks, RL90 inhibits the catalytic cycle of the enzyme itself. Preclinical research has demonstrated that RL90 exhibits selective growth inhibition against tamoxifen-resistant breast cancer cell lines, specifically variant sub-lines of MCF-7 such as TamR3 and TamC3. Treatment with RL90 induces S-phase selective DNA damage and histone H2AX phosphorylation. It serves as a lead compound for the development of novel therapeutic agents targeting endocrine-resistant malignancies.

Other names

2,6-bis(pyridin-3-ylmethylene)-cyclohexanone2,6-bis(3-pyridinylmethylene)cyclohexanone