ACY-738

製品コードS8648 バッチS864802

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₄N₄O₂

分子量

270.29

CAS No.

1375465-91-0

Solubility (25°C)*

体外

DMSO

54 mg/mL (199.78 mM)

Ethanol

1 mg/mL (3.69 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.700mg/ml (9.99mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.400mg/ml (1.48mM)

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
in vivo	ACY-738 induces dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors in novel, but not familiar environments. This compound has the antidepressant-like properties. Elimination of this chemical from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/ml after 2 h. It rapidly distributes to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues^[1]. This agent decreases several characteristics of SLE (Systemic lupus erythematosus) in NZB/W mice by dictating B cell development in the bone marrow. Its treatment increases the percentage of B cells in early developmental stages, while decreasing the percentage of cells in late pre-B cell fraction F. The compound's regulation of BM B cell development could be due to regulation developmental checkpoints known to be dysfunctional during SLE^[2].

製品説明

ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.

in vivo

ACY-738 induces dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors in novel, but not familiar environments. This compound has the antidepressant-like properties. Elimination of this chemical from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/ml after 2 h. It rapidly distributes to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues^[1]. This agent decreases several characteristics of SLE (Systemic lupus erythematosus) in NZB/W mice by dictating B cell development in the bone marrow. Its treatment increases the percentage of B cells in early developmental stages, while decreasing the percentage of cells in late pre-B cell fraction F. The compound's regulation of BM B cell development could be due to regulation developmental checkpoints known to be dysfunctional during SLE^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Undifferentiated RN46A-B14 cells
	濃度	2.5 μM
	反応時間	4 h
	実験の流れ	Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, are grown. They are treated with 2.5 μM ACY-738, this compound, tubastatin A, or 0.6 μM TSA, or vehicle (0.1% DMSO) for 4 h. Samples are processed using Epigentek histone extraction kit and quantified using protein assay.
動物実験	動物モデル	Male NIH Swiss mice
	投薬量	5 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/23954848/
https://pubmed.ncbi.nlm.nih.gov/26604012/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Aggresome assembly at the centrosome is driven by CP110-CEP97-CEP290 and centriolar satellites [ Nat Cell Biol, 2022, 24(4):483-496]	PubMed: 35411088
Histone deacetylase 6 plays an important role in TGF-β-induced murine Treg cell differentiation by regulating cell proliferation [ Sci Rep, 2022, 12(1):22550]	PubMed: 36581745
The CP110-CEP97-CEP290 module orchestrates a centriolar satellite dependent response to proteotoxic stress [ bioRxiv, 2020, 10.1101/2020.12.20.423672]	PubMed: None
HDAC6 dysfunction contributes to impaired maturation of adult neurogenesis in vivo: vital role on functional recovery after ischemic stroke [ J Biomed Sci, 2019, 26(1):27]	PubMed: 30999900

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。