Drug intelligence / Profile preview

ML-60218

Development stage
Preclinical
Lead developer
National Institutes of Health
Modality
Small Molecules
Administration
Oral
01

Overview

ML-60218 is a cell-permeable, small molecule inhibitor of RNA polymerase III (Pol III). It was identified through the NIH Molecular Libraries Probe Production Centers Network (MLPCN) as a potent and selective inhibitor of Pol III-mediated transcription. By blocking the synthesis of small non-coding RNAs, such as tRNAs and 5S rRNAs, ML-60218 interferes with essential cellular processes including protein synthesis and cell growth. Preclinical research has demonstrated its potential in oncology, specifically in suppressing the proliferation of human pancreatic adenocarcinoma cells and inducing apoptosis, especially when used in synergistic combination with histone deacetylase (HDAC) inhibitors. It is primarily utilized as a chemical probe to investigate the regulatory roles of Pol III in development and malignant transformation.

02

Targets

Pol II (RNA polymerase II elongation factors)Pol III (Dna-directed RNA polymerase III)Pol I (RNA polymerase I)

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