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577784-91-9

中文名稱 RNA Polymerase III Inhibitor
英文名稱 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 結(jié)構(gòu)式 577784-91-9 結(jié)構(gòu)式

基本信息

中文別名
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
英文別名
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]-

物理化學(xué)性質(zhì)

儲(chǔ)存條件= -70C
溶解度Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 5 mg/ml with warming)
形態(tài)類白色固體
顏色Off-white
穩(wěn)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.
InChI1S/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
InChIKeyBVBDTTLISMIOJY-UHFFFAOYSA-N
SMILES[S](=O)(=O)(Nc2[n](nc(c2)c3[s]c4c(c3C)cc(cc4)Cl)C)c1c(cccc1)Cl

安全數(shù)據(jù)

WGK GermanyWGK 1
存儲(chǔ)類別10 - Combustible liquids

常見(jiàn)問(wèn)題列表

生物活性
ML-60218 是一種廣譜 RNA pol III 抑制劑,對(duì)釀酒酵母和人類 RNA pol III 的 IC50 分別為 32 和 27 μM。ML-60218 破壞已經(jīng)組裝好的病毒體,并且在不需要重新轉(zhuǎn)錄細(xì)胞 RNA 的情況下阻礙新病毒體的形成。
體外研究

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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