577784-91-9

577784-91-9 structure

Name: RNA Polymerase III Inhibitor
Chemical Name: 2-chloro-N-[5-(5-chloro-3-methyl-1-benzothiophen-2-yl)-2-methylpyrazol-3-yl]benzenesulfonamide
CAS Number: 577784-91-9
Molecular Formula: C₁₉H₁₅Cl₂N₃O₂S₂
Molecular Weight: 452.377
Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA/RNA Synthesis
Create Date: 2016-01-25 09:34:26
Modify Date: 2024-01-02 19:05:02
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].

Name	2-chloro-N-[5-(5-chloro-3-methyl-1-benzothiophen-2-yl)-2-methylpyrazol-3-yl]benzenesulfonamide
Synonyms	RNA Polymerase III Inhibitor 2-Chloro-N-[3-(5-chloro-3-methyl-1-benzothiophen-2-yl)-1-methyl-1H-pyrazol-5-yl]benzenesulfonamide N1-[3-(5-chloro-3-methylbenzo[b]thiophen-2-yl)-1-methyl-1H-pyrazol-5-yl]-2-chlorobenzene-1-sulfonamide Benzenesulfonamide, 2-chloro-N-[3-(5-chloro-3-methylbenzo[b]thien-2-yl)-1-methyl-1H-pyrazol-5-yl]- ML-60218

Description	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].
Related Catalog	Research Areas >> Cancer Research Areas >> Infection Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis
In Vitro	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].
References	[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.

Density	1.5±0.1 g/cm3
Boiling Point	632.3±65.0 °C at 760 mmHg
Molecular Formula	C₁₉H₁₅Cl₂N₃O₂S₂
Molecular Weight	452.377
Flash Point	336.2±34.3 °C
Exact Mass	450.998260
PSA	100.61000
LogP	6.83
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.715

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