N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺 T6325

Product Introduction
Bioactivity


英文名: PCI-34051

描述: PCI-34051 是一种有效的选择性的HDAC8抑制剂，IC50为 10 nM。

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.

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.

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]。

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

溶解度: DMSO : 29.6 mg/mL (100 mM)
1eq. NaOH : 5.9 mg/mL (20 mM)


关键字: PCI34051 | Apoptosis | inhibit | HDAC | Histone deacetylases | Inhibitor | PCI-34051

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途