Tubacin

製品コードS2239 バッチS223902

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

C₄₁H₄₃N₃O₇S

分子量

721.86

CAS No.

537049-40-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (138.53 mM)

Water

Insoluble

Ethanol

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。	5.000mg/ml (6.93mM)
	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。	1.250mg/ml (1.73mM)

* <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	Tubacinは、in vitroアッセイでIC50が4 nMの、非常に強力で選択的な可逆性細胞透過性HDAC6阻害剤であり、HDAC1に対して約350倍の選択性を示します。Tubacinは、ウイルスRNA合成の減少を介して、日本脳炎ウイルスの複製を減少させます。
in vitro	Tubacin, without directly stabilizing microtubules, induces an increase in α-tubulin acetylation with EC50 of 2.5 μM in A549 cells. This compound inhibits HDAC6-mediated α-tubulin deacetylation, and inhibits the migration of both wild-type and HDAC6-overexpressing cells. It in combination synergistically enhances tubulin acetylation. This chemical significantly inhibits both drug-sensitive and drug–resistant MM cell growth with IC50 of 5–20 μM, and induces cell apoptosis by activation of caspases.
in vivo	In chick embryos, inhibition of HDAC6 activity by Tubacin reduces the formation of new blood vessels in matrigel/nylon mesh. In angioreactors implanted in mice, this compound also impairs the formation of new blood vessels.
特徴	The first known selective inhibitor of α-tubulin deacetylation.

プロトコル(参考用のみ)

キナーゼアッセイ	Enzyme Inhibition Assay
キナーゼアッセイ	Enzyme inhibition assays are performed using the Reaction Biology HDAC Spectrum platform. The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays used isolated recombinant human protein; HDAC3/NcoR2 complex is used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10, and 11 assays is a fluorogenic peptide from p53 residues 379-382 (RHKKAc); substrate for HDAC8 is fluorogenic diacyl peptide based on residues 379-382 of p53 (RHKAcKAc). Acetyl-Lys(trifluoroacetyl)-AMC substrate is used for HDAC4, 5, 7, and 9 assays. Compounds are dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A (TSA) is tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values are extracted by curve-fitting the dose/response slopes.
細胞アッセイ	細胞株	Drug-sensitive (MM.1S, U266, INA-6, and RPMI8226) and drug-resistant (RPMI-LR5 and RPMI-Dox40) MM cell lines
	濃度	~20 μM
	反応時間	72 hours
	実験の流れ	The inhibitory effect of this compound on MM cell growth is assessed by measuring the MTT dye absorbance. All experiments are performed in quadruplicate.
動物実験	動物モデル	Athymic nude mice implanted with angioreactors
	投薬量	--
	投与方法	Tubacin is filled in semiclosed angioreactors, and then implanted into the mice.

参考

https://pubmed.ncbi.nlm.nih.gov/20614936/
https://pubmed.ncbi.nlm.nih.gov/12677000/
https://pubmed.ncbi.nlm.nih.gov/15867388/

https://pubmed.ncbi.nlm.nih.gov/15937109/
https://pubmed.ncbi.nlm.nih.gov/21359602/

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カスタマーフィードバック

: Data from [Data independently produced by , , Nat Biotechnol, 2015, 33(4): 415-23 ]

: Data from [Data independently produced by , , Oncogene, 2016, 35(18):2333-44]

: Data from [Data independently produced by , , J Biol Chem, 2016, 291(10):5396-405]

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：

Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5]	PubMed: 38823394
Microtubule acetylation and PERK activation facilitate eribulin-induced mitochondrial calcium accumulation and cell death [ Cell Mol Life Sci, 2024, 82(1):32]	PubMed: 39741209
Optogenetically Induced Microtubule Acetylation Unveils the Molecular Dynamics of Actin-Microtubule Crosstalk in Directed Cell Migration [ bioRxiv, 2024, 2024.12.01.626286]	PubMed: 39677776
Selective inhibition of HDAC6 promotes bladder cancer radiosensitization and mitigates the radiation-induced CXCL1 signalling [ Br J Cancer, 2023, 10.1038/s41416-023-02195-0]	PubMed: 36810912
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells [ Int J Mol Sci, 2023, 24(5)4720]	PubMed: 36902164
MicroRNA-22 represses glioma development via activation of macrophage-mediated innate and adaptive immune responses [ Oncogene, 2022, 10.1038/s41388-022-02236-7]	PubMed: 35279703
Dual Blockade of Misfolded Alpha-Sarcoglycan Degradation by Bortezomib and Givinostat Combination [ Front Pharmacol, 2022, 13:856804]	PubMed: 35571097
Hypoxia Selectively Increases a SMAD3 Signaling Axis to Promote Cancer Cell Invasion [ Cancers (Basel), 2022, 14(11)2751]	PubMed: 35681731
Targeting cancer cell plasticity by HDAC inhibition to reverse EBV-induced dedifferentiation in nasopharyngeal carcinoma [ Signal Transduct Target Ther, 2021, 6(1):333]	PubMed: 34482361
A protocol to visualize cytosolic aggresome-like bodies using confocal microscopy [ STAR Protoc, 2021, 2(3):100674]	PubMed: 34337443

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。