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577784-91-9

中文名称 RNA Polymerase III Inhibitor
英文名称 RNA Polymerase III Inhibitor
CAS 577784-91-9
分子式 C19H15Cl2N3O2S2
分子量 452.38
MOL 文件 577784-91-9.mol
577784-91-9 结构式 577784-91-9 结构式

基本信息

中文别名
化合物ML-60218
化合物ML-60218,10 MM DMSO 溶液
2-氯-N-(3-(5-氯-3-甲基苯并[B]噻吩-2-基)-1-甲基-1H-吡唑-5-基)苯磺酰胺
英文别名
RNA Polymerase III Inhibitor
RNA Polymerase III Inhibitor - CAS 577784-91-9 - Calbiochem
InSolution RNA Polymerase III Inhibitor - CAS 577784-91-9 - Calbiochem
2-chloro-N-[5-(5-chloro-3-methyl-1-benzothiophen-2-yl)-2-methylpyrazol-3-yl]benzenesulfonamide
Benzenesulfonamide, 2-chloro-N-[3-(5-chloro-3-methylbenzo[b]thien-2-yl)-1-methyl-1H-pyrazol-5-yl]-

物理化学性质

储存条件= -70C
溶解度Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 5 mg/ml with warming)
形态类白色固体
颜色Off-white
稳定性Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.

常见问题列表

生物活性
ML-60218 是一种广谱 RNA pol III 抑制剂,对酿酒酵母和人类 RNA pol III 的 IC50 分别为 32 和 27 μM。ML-60218 破坏已经组装好的病毒体,并且在不需要重新转录细胞 RNA 的情况下阻碍新病毒体的形成。
体外研究

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.
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.

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