Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PCI-34051 是一种有效的选择性的HDAC8抑制剂,IC50为 10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 223 | 现货 | ||
5 mg | ¥ 495 | 现货 | ||
10 mg | ¥ 886 | 现货 | ||
25 mg | ¥ 1,850 | 现货 | ||
50 mg | ¥ 3,550 | 现货 | ||
100 mg | ¥ 5,220 | 现货 | ||
500 mg | ¥ 10,900 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 549 | 现货 |
产品描述 | PCI-34051 is an effective and selective HDAC8 inhibitor (IC50: 10 nM). |
靶点活性 | HDAC8:10 nM |
体外活性 | PCI-34051 has a good potency for HDAC8 (Ki: 10 nM). PCI-34051 has high specificity (about 5-fold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 has higher 200-fold selectivity than HDAC1/6 and higher 1000-fold selectivity than HDAC2/3//10. PCI-34051 inhibits ovarian tumor line OVCAR-3 (GI50: 6 μM) and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 (<25 μM) at 24 hours nor at earlier time points. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours. PCI-34051 does not stimulate Bid cleavage. While J.RT3-T.5 and P116 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line shows a marked decrease in the extent of PCI-34051-induced apoptosis. Furthermore, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria. |
体内活性 | 给予PCI-34051和Dexamethasone可以减少哮喘中的嗜酸性炎症和气道高反应性,从而减少气道重塑[2]。 |
激酶实验 | Histone deacetylase activity:For PCI-34051 characterization, measurements are performed in a reaction volume of 100 μL using 96-well assay plates in a fluorescence plate reader. For each isozyme. The HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% dimethyl sulfoxide, pH7.4, supplemented with bovine serum albumin at concentrations of 0-0.05%) is mixed with PCI-34051 at various concentrations and allowed to incubate for 15 min. Trypsin is added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-amino-4-methyl coumarin is added to a final concentration of 25-100 μM to initiate the reaction. After a 30 min lag time, the fluorescence is measured over a 30 min time frame using an excitation wavelength of 335 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. |
细胞实验 | Cell lines: A549 cell line,Ovcar-3 cell line. Concentrations: 5 μM. Incubation Time: 24 hours. Method: Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times,and growth is monitored at the end of PCI-34051 exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer.PCI-34051 is assayed in triplicate wells in 96-well plates.The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from the nonlinear regression using a four-parameter logistic equation. |
别名 | N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺, PCI 34051 |
分子量 | 296.32 |
分子式 | C17H16N2O3 |
CAS No. | 950762-95-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 29.6 mg/mL (100 mM)
1eq. NaOH: 5.9 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / 1eq. NaOH | 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL | 84.3683 mL |
5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | 16.8737 mL | |
10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL | 8.4368 mL | |
20 mM | 0.1687 mL | 0.8437 mL | 1.6874 mL | 4.2184 mL | |
DMSO | 50 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6874 mL |
100 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8437 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。
PCI-34051 950762-95-5 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC PCI34051 inhibit N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺 Histone deacetylases Inhibitor PCI 34051 inhibitor