Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HPOB 是一种高选择性HDAC6抑制剂,IC50为 56 nM,其选择性是其他 HDAC 的 30 倍以上。它提高 DNA 损伤抗癌药物在转化细胞中的有效性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 374 | 现货 | ||
10 mg | ¥ 598 | 现货 | ||
25 mg | ¥ 1,235 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs. |
靶点活性 | HDAC6:56 nM |
体外活性 | 在负荷CWR22人前列腺癌异种移植物的小鼠体内,HPOB(300 mg/kg/day)与SAHA联用可抑制已生成肿瘤的生长,而单独使用时则无明显抑制作用. |
体内活性 | 在HFS细胞中,HPOB对依托泊苷,阿霉素,或SAHA诱导的转化细胞死亡具有增强作用。在转化细胞中,通过凋亡通路HPOB也会增强依托泊苷诱导的转化细胞死亡。在正常(HFS)和转化的(LNCaP,A549,和U87)细胞中,HPOB诱导α-微管蛋白,但不影响组蛋白,抑制细胞生长,但不影响细胞活性。 |
激酶实验 | In Vitro Enzymatic Assay for Histone Deacetylases: In vitro activities of the 11 recombinant human zinc-dependent HDAC enzymes are detected by ?uorigenic release of 7-amino-4-methylcoumarin from substrate upon deacetylase enzymatic activity. A series of dilutions of the unique HDAC6 compound, tubacin, and SAHA are prepared with 10% DMSO in HDAC assay buffer, and 5 μL of the dilution was added to a 50-μL reaction so that the ?nal concentration of DMSO is 1% in all of the reactions. The enzymatic reactions are conducted in duplicate at 37 °C for 30 min in a 50-μL mixture containing HDAC assay buffer, 5 μg BSA, an HDAC substrate, an HDAC enzyme, and a test compound. After enzymatic reactions, 50 μL of 2× HDAC developer is added to each well, and the plate is incubated at room temperature for an additional 15 min. Fluorescence intensity is measured at an excitation of 360 nm and an emission of 460 nm using a Synergy microplate reader. Negative (no enzyme, no inhibitor, a drug with no HDAC inhibition activity) and positive controls (known HDAC inhibitor SAHA) are included in the assays. IC50 is determined at the drug concentration that results in 50% reduction of HDAC activity compared with the control. |
细胞实验 | Normal (HFS) and transformed (LNCaP, A549, and U87) cells are cultured with indicated doses of HPOB for 72 h. Five micromolars SAHA is a positive control.Graphs were constructed using Prism 5. (Only for Reference) |
分子量 | 314.34 |
分子式 | C17H18N2O4 |
CAS No. | 1429651-50-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 36 mg/mL (114.5 mM)
DMSO: 58 mg/mL (184.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.1813 mL | 15.9063 mL | 31.8127 mL | 79.5317 mL |
5 mM | 0.6363 mL | 3.1813 mL | 6.3625 mL | 15.9063 mL | |
10 mM | 0.3181 mL | 1.5906 mL | 3.1813 mL | 7.9532 mL | |
20 mM | 0.1591 mL | 0.7953 mL | 1.5906 mL | 3.9766 mL | |
50 mM | 0.0636 mL | 0.3181 mL | 0.6363 mL | 1.5906 mL | |
100 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
HPOB 1429651-50-2 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC cells anticancer Histone deacetylases tumor A549 U87 Inhibitor inhibit LNCaP CWR22 selective inhibitor