For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I032429 |
| CAS Number | 577784-91-9 |
| Synonyms | 2-chloro-N-[5-(5-chloro-3-methyl-1-benzothiophen-2-yl)-2-methylpyrazol-3-yl]benzenesulfonamide |
| Molecular Formula | C19H15Cl2N3O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H15Cl2N3O2S2/c1-11-13-9-12(20)7-8-16(13)27-19(11)15-10-18(24(2)22-15)23-28(25,26)17-6-4-3-5-14(17)21/h3-10,23H,1-2H3 |
| InChIKey | BVBDTTLISMIOJY-UHFFFAOYSA-N |
| SMILES | CC1=C(SC2=C1C=C(C=C2)Cl)C3=NN(C(=C3)NS(=O)(=O)C4=CC=CC=C4Cl)C |
| 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. |
