Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Procaine (Vitamin H3) 是DNA 脱甲基剂,是一种酯类局部麻醉剂。它起效缓慢,作用持续时间短,主要用于浸润麻醉、周围神经阻滞和脊髓阻滞。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 Procaine hydrochloride 的水溶性和稳定性通常比游离态更好。
产品描述 | Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. |
体外活性 | Procaine显著降低了HLE、HuH7和HuH6细胞的活性。Procaine在对HLE细胞实验时观察到S/G2/M周期转换受阻、形态学变化如空泡化,但凋亡率并未增加。Procaine处理后因DNA过度甲基化而转录抑制的基因被去甲基化并重新激活。Procaine对人类肝癌细胞具有生长抑制和去甲基化作用[2]。 |
体内活性 | Procaine 在体内对异种移植瘤具有生长抑制和脱甲基作用[2]。 |
激酶实验 | Biochemical Assays: Compound potency is also assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, PRC2 containing either EZH1 (160 pM), wt EZH2 (40 pM), or Y641N mutant EZH2 (80 pM, both EZH2 prepared in-house) is pre-incubated with 3H-SAM (0.9 μM), 2 μM H3K27me3 activating peptide (H2N-RKQLATKAAR(Kme3)SAPATGGVKKP-amide) and compounds (as 10 point duplicate dose response titrations) for 120 min in a buffer consisting of 50 mM Tris (pH 8.5), 1 mM DTT, 0.07 mM Brij-35, 0.1% BSA, and 0.8% DMSO in a total volume of 12.5 μl in a black 384 well plate. Reaction is initiated with biotinylated H3 substrate peptides (H3K27me1 for wt EZH2, H3K27me2 for Y641N mutant EZH2; H2N-RKQLATKAAR(Kmen)SAPATGGVKKP-NTPEGBiot) as a 2 μM stock in 12.5 μL and allowed to react at room temperature for 5 h. Quenching is accomplished by addition of 20 μl of STOP solution (50 mM Tris (pH 8.5), 200 mM EDTA, 2 mM SAH). 35 μL of the quenched solution is transferred to Streptavidin Flashplates, incubated overnight, washed, and read in a TopCount Reader. For titrations all compound dilutions are in DMSO, final DMSO concentrations are 0.8% (v/v), and turnover is kept to less than < 5%. IC50s are calculated using non-linear least square four parameter fits (GraphPad 6.0). |
细胞实验 | For apoptosis analysis, the TUNEL assay is performed on HLE cells treated with no drug(control), or 1 μM of DAC(5-aza-2'-deoxycytidine), or 1 mM of PCA(procaine), or 1 mM of PCAA(procainamide) for 96 h. The proportion of TUNEL-positive cells was calculated by counting at least 500 cells randomly. All assays were carried out in triplicate. (Only for Reference) |
别名 | Duracaine, Spinocaine, 普鲁卡因, Novocaine, Vitamin H3, 奴夫卡因 |
分子量 | 236.31 |
分子式 | C13H20N2O2 |
CAS No. | 59-46-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 47 mg/mL (198.89 mM)
Ethanol: 43 mg/mL(182 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 4.2317 mL | 21.1586 mL | 42.3173 mL | 105.7932 mL |
5 mM | 0.8463 mL | 4.2317 mL | 8.4635 mL | 21.1586 mL | |
10 mM | 0.4232 mL | 2.1159 mL | 4.2317 mL | 10.5793 mL | |
20 mM | 0.2116 mL | 1.0579 mL | 2.1159 mL | 5.2897 mL | |
50 mM | 0.0846 mL | 0.4232 mL | 0.8463 mL | 2.1159 mL | |
100 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0579 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。
Procaine 59-46-1 Cell Cycle/Checkpoint Chromatin/Epigenetic DNA Damage/DNA Repair Membrane transporter/Ion channel Histone Demethylase DNA/RNA Synthesis Sodium Channel targets Inhibitor Duracaine onset inhibit multiple Spinocaine 普鲁卡因 Novocaine Vitamin H3 奴夫卡因 duration inhibitor