RNA Polymerase III Inhibitor

Description

ML60218 (CAS 577784-91-9) is a broad spectrum inhibitor of RNA polymerase III from?S. Cerevisiae?as well as from human cells, IC50=32?mM and 27?mM respectively.1?? Combined treatment with ML-60218 and an HDAC inhibitor caused augmented suppression of colony formation, induction of cell cycle arrest and apoptotic cell death in human pancreatic adenocarcinoma cells.2

General Description

A cell-permeable indazolo-sulfonamide compound that displays broad-spectrum inhibitory activity against RNA Polymerase III (IC₅₀ = 27 and 32 μM for human and S. cerevisiae RNA Pol III, respectively). Inhibits cell growth in yeast by preventing RNA Pol III-mediated tRNA transcription. Also available as a 25 mM solution in DMSO (Cat. No. 557404).

Biochem/physiol Actions

Product does not compete with ATP.

References

1) Wu?et al.?(2003),?Novel small-molecule inhibitors of RNA polymerase III; Eukaryot. Cell,?2?256 2) Yee?et al.?(2012),?Targeting developmental regulators of zebrafish exocrine pancreas as a therapeutic approach in human pancreatic cancer; Biol. Open,?1(4)?295