化合物BMH-21 T1767

Product Introduction
Bioactivity


英文名: BMH-21

描述: BMH-21 是一种小分子 DNA 嵌入剂，可结合核糖体 DNA 并抑制 RNA 聚合酶 I (Pol I) 转录，具有抗癌活性。

细胞实验: The cells are maintained at 37 °C in a humidified atmosphere containing 5% CO2. U2OS osteosarcoma cells are cultured in DMEM supplemented with 15% fetal bovine serum. Cells are plated in 96-well plates at a density of 10000 cells/well in triplicate and incubated for 48 h with the compounds. Viability is determined using WST-1 cell proliferation reagent. (Only for Reference)

激酶实验: [14C]-monosaccharide uptake inhibition experiments: Stable cell lines over-expressing hSGLT-1, -2, -4, -5 or -6 or rSGLT-1 or -2 are used for the sodium-dependent monosaccharide transport inhibition assay. Cells are pre-incubated in 200 μL uptake buffer (10 mM HEPES, 137 mM NaCl, 5.4 mM KCl, 2.8 mM CaCl2, 1.2 mM MgCl2, 50 μg/ml Gentamycin, 0.1% BSA) for 25 minutes at 37°C. 10 μM Cytochalasin B and test compound is added at different concentrations 15 minutes before the initiation of the uptake experiment. The uptake reaction is started by the addition of 0.6 μCi [14C]-labelled monosaccharide i.e. [14C]-labelled AMG, glucose, fructose, mannose or myo-inositol, in 0.1 mM AMG (or the respective non-radioactive monosaccharide). After incubation for 60 minutes (hSGLT-5), 90 minutes (hSGLT-4) or 4 hours (hSGLT-2) at 37°C, the cells are washed three times with 300 μL PBS and then lysed in 0.1 N NaOH with intermittent shaking for 5 minutes. The lysate is mixed with 200 μL MicroScint 40 and shaken for 15 minutes and counted for radioactivity in the TopCount NXT. For SGLT-4 and SGLT-5 assays cells are pre-incubated in pre-treatment buffer (uptake buffer containing choline chloride instead of NaCl) for 25 minutes prior to addition of uptake buffer.

体外活性: 在小鼠异种移植物中,BMH-21可抑制肿瘤生长.

体内活性: 在U2OS癌症细胞系中,BMH-21可使NCL易位（IC50：0.07 μM）和RPA194降解（IC50：0.05 μM）。BMH-21引起RPA194依赖性的蛋白酶体破坏,RPA194为Pol I全复合物的大催化亚基蛋白。通过引起核仁应激,BMH-21也可有效抑制细胞活性。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 2 mg/mL (5.54 mM)
DMSO : 5 mg/mL (13.87 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: nucleolus | polymerase | damage | intercalation | transcription | RNA | BMH 21 | response | DNA | BMH-21 | inhibit | Inhibitor | DNA/RNA Synthesis

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