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ACY-775
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ACY-775
CAS No. : 1375466-18-4
MCE 站:ACY-775
产品活性:ACY-775 是一个有效的,选择性强的组蛋白脱乙酰酶 6 (HDAC6) 抑制剂 IC50 值为 7.5 ?nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:HDAC
In Vitro: In vehicle-treated cells, α-tubulin is mainly presented in the deacetylated form, while histone 3 is clearly acetylated. Upon treatment with ACY-775, a clear enhancement of the acetylation of α-tubulin is visible, while histone acetylation remains unaltered. Acetylation of α-tubulin is visualized by immunofluorescence and the intensity in the neurites of the neurons is quantified and normalized to the length of the fluorescent signal. In vehicle-treated DRG neurons, acetylated α-tubulin is already present. Upon treatment with ACY-775 the signal intensity of acetylated α-tubulin increases significantly. Significant increase in motility of mitochondria and also the total number of mitochondria within the neurites are observed compare with vehicle-treated DRG neurons. A significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compare with vehicle-treated cells.
In Vivo: Biodistribution profiles of ACY-738, ACY-775, and tubastatin A are examined after acute dosing at 5 or 50?mg/kg over 2?h. At t=30?min after acute 50?mg/kg injection, respective plasma levels of ACY-738 and ACY-775 are 515?ng/mL (1.9?μM) and 1359?ng/mL (4.1?μM). Elimination from plasma is rapid, with plasmatic half-life of 12?min and concentration below 10?ng/mL after 2?h. Nevertheless, areas under concentration time curves for brain and plasm calculated over 2?h for both ACY-738 and ACY-775 lead to ratios >1. When ACY-738 (5?mg/kg) or ACY-775 (50?mg/kg) are administered repeatedly in wild-type mice at 24?h, 4?h, and 30?min before killing, significant increases in α-tubulin acetylation are observed in all tested brain regions.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-Cardiovascular Disease Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Trichostatin A | 4-Phenylbutyric acid | Valproic acid | Entinostat | Sulforaphane | Romidepsin | RGFP966 | Tasquinimod | Corin | Tacedinaline | Dacinostat | ITSA-1 | SIS17 | Tubastatin A Hydrochloride | WT-161 | Givinostat hydrochloride monohydrate | Pyroxamide | BRD-6929 | Bufexamac | HDAC8-IN-1 | Scriptaid | Sinapinic acid | Apicidin | BML-210 | M344 | Droxinostat | HDACs/mTOR Inhibitor 1 | CG347B
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