Tubacin

製品コードS2239 バッチS223901

印刷

化学情報

Chemical Structure 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
* <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 is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis.
in vitro Tubacin, without directly stabilizing microtubules, induces an increase in α-tubulin acetylation with EC50 of 2.5 μM in A549 cells. Tubacin inhibits HDAC6-mediated α-tubulin deacetylation, and inhibits the migration of both wild-type and HDAC6-overexpressing cells. [2] Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. [3] Tubacin 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. [4]
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, Tubacin also impairs the formation of new blood vessels. [5]
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
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 bortezomib and/or tubacin on MM cell growth is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (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.

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：

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
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
Protein acetylation derepresses Serotonin Synthesis to potentiate Pancreatic Beta-Cell Function through HDAC1-PKA-Tph1 signaling [ Theranostics, 2020, 10(16):7351-7368] PubMed: 32641996
Chaperone-Assisted Mitotic Actin Remodeling by BAG3 and HSPB8 Involves the Deacetylase HDAC6 and Its Substrate Cortactin [ Int J Mol Sci, 2020, 22(1)E142] PubMed: 33375626

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。