Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ACY-738 对重组 HDAC6 具有抑制活性IC50值为 1.7 nM。它也可抑制 HDAC1、HDAC2 和 HDAC3 的活性,IC50值分别为 94、128 和 218 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
2 mg | ¥ 722 | 现货 | ||
5 mg | ¥ 1,470 | 现货 | ||
10 mg | ¥ 2,310 | 现货 | ||
25 mg | ¥ 3,890 | 现货 | ||
50 mg | ¥ 5,580 | 现货 | ||
100 mg | ¥ 7,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,090 | 现货 |
产品描述 | ACY-738 demonstrates inhibitory activity against recombinant HDAC6 (IC50: 1.7 nM), with respective average selectivity over class I HDACs being 100-fold. |
靶点活性 | HDAC6:1.7 nM |
体外活性 | ACY-738 increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells at the concentration of 2.5?μM. The effect that ACY-738 (10 μM) induces cell death is similar to LBH589 and FK228. |
体内活性 | ACY-738 (5?mg/kg) leads to obviously increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50?mg/kg) cannot produce an enhancement of locomotor activity in WT mice tested in a home cage environment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. It also significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. |
激酶实验 | Recombinant kinase domain of EGFR L858R and T790M-L858R mutants are incubated with EGF816 to confirm covalent modification of EGFR and site of adduction. Recombinant enzyme is incubated at room temperature with a 20-fold molar excess of compound in 40 mM Tris, pH 8, 500 mM NaCl, 1% glycerol, 5 mM TCEP for 1 h. The reaction is quenched by addition of dithiothreitol (DTT, 80-fold excess to compound) and transfer to ice. A third of the reaction (10 μL) is processed for intact MS by adding an equal volume of 6 M Guan HCl, 100 mM Tris, pH 8, 20 mM DTT, 10 mM TCEP and incubating at room temperature for 15 min. Intact MS analysis is performed on an Agilent 6520 QToF mass spectrometer equipped with a dual spray ion source (IS of 4500 V, fragmentor of 250 V, fas temp of 350°C, and skimmer of 75 V). The samples are injected onto a PLRP-S column (2.1 mm × 50 mm), heated to 60°C, and desalted for 2 min at 500 μL/min and 3% B prior to elution with a fast gradient of 3-50% B in 3 min (B, 0.1% formic acid). The data are analyzed in MassHunter for automatic peak selection, integration, and spectral deconvolution with a mass range of 15?000-75?000 Da. |
别名 | ACY 738 |
分子量 | 270.29 |
分子式 | C14H14N4O2 |
CAS No. | 1375465-91-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (184.99 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.6997 mL | 18.4986 mL | 36.9973 mL | 92.4932 mL |
5 mM | 0.7399 mL | 3.6997 mL | 7.3995 mL | 18.4986 mL | |
10 mM | 0.37 mL | 1.8499 mL | 3.6997 mL | 9.2493 mL | |
20 mM | 0.185 mL | 0.9249 mL | 1.8499 mL | 4.6247 mL | |
50 mM | 0.074 mL | 0.37 mL | 0.7399 mL | 1.8499 mL | |
100 mM | 0.037 mL | 0.185 mL | 0.37 mL | 0.9249 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。
ACY-738 1375465-91-0 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC ACY738 Histone deacetylases inhibit ACY 738 Inhibitor inhibitor