RNA Polymerase III Inhibitor
- CAS号:577784-91-9
- 英文名:RNA Polymerase III Inhibitor
- 中文名:RNA Polymerase III Inhibitor
- CBNumber:CB63136764
- 分子式:C19H15Cl2N3O2S2
- 分子量:452.38
- MOL File:577784-91-9.mol
- 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 :Off-white solid
- 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.
RNA Polymerase III Inhibitor性质、用途与生产工艺
- 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。
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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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