ML-60218_product_DataBase

Bioactivity

ML-60218 is a broad-spectrum RNA pol III inhibitor, with IC50s of 32 and 27 μM for Saccharomyces cerevisiae and human. ML-60218 disrupts already assembled viroplasms and to hamper the formation of new ones without the need for de novo transcription of cellular RNAs[1][2].

Invitro

Combination of SAHA and ML-60218 produces enhanced suppression of proliferation in human pancreatic adenocarcinoma by impairing cell cycle progression and inducing apoptosis. ML-60218 reverses SAHA-stimulated tRNA expression in PANC-1 and BxPC-3 cells. ML-60218 enhances the ability of HDAC inhibitors to induce apoptosis and cell cycle arrest[2].In in vitro transcription assays with purified double-layered particles (DLPs), ML-60218 shows dose-dependent inhibitory activity, indicating the viral nature of its target. ML-60218 is found to interfere with the formation of higher-order structures of VP6, the protein forming the DLP outer layer, without compromising its ability to trimerize. Electron microscopy of ML-60218-treated DLPs shows dose-dependent structural damage. ML-60218-mediated (10 μM ) viroplasm disruption causes NSP5 dephosphorylation[3].

Name

ML-60218

CAS

577784-91-9

Formula

C19H15Cl2N3O2S2

Molar Mass

452.38

Appearance

Liquid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Wu L, et al. Novel small-molecule inhibitors of RNA polymerase III. Eukaryot Cell. 2003;2(2):256-264. [2]. Yee NS, et al. Targeting developmental regulators of zebrafish exocrine pancreas as a therapeutic approach in human pancreatic cancer. Biol Open. 2012;1(4):295-307. [3]. Eichwald C, et al. Identification of a Small Molecule That Compromises the Structural Integrity of Viroplasms and Rotavirus Double-Layered Particles. J Virol. 2018;92(3):e01943-17. Published 2018 Jan 17.

PeptideDB

ML-60218

CAS: 577784-91-9 F: C19H15Cl2N3O2S2 W: 452.38