受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C41H43N3O7S |
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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) |
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* <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. |
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. |
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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. |
キナーゼアッセイ | Enzyme Inhibition Assay | |
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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. |
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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. |
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]
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。
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