| 名稱 | Tubacin |
| 描述 | Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1. |
| 細(xì)胞實(shí)驗(yàn) | Cell lines: Drug-sensitive (MM.1S,U266,INA-6,and RPMI8226) and drug-resistant (RPMI-LR5 and RPMI-Dox40) MM cell lines. Concentrations: ~20 μM. Incubation Time: 72 hours. Method: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. |
| 激酶實(shí)驗(yàn) | 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. |
| 動(dòng)物實(shí)驗(yàn) | Animal Models: Athymic nude mice implanted with angioreactorsFormulation: DMSODosages: --Administration: Tubacin is filled in semiclosed angioreactors, and then implanted into the mice. |
| 體外活性 | Tubacin不直接穩(wěn)定微管，通過提高A549細(xì)胞中α-微管蛋白乙?；剑‥C50為2.5μM）發(fā)揮作用。Tubacin抑制HDAC6介導(dǎo)的α-微管蛋白去乙?；饔茫⒛茏柚挂吧图癏DAC6過表達(dá)細(xì)胞的遷移。與紫杉醇聯(lián)合使用時(shí)，Tubacin可協(xié)同增強(qiáng)微管蛋白乙?；Ｍ瑫r(shí)，Tubacin顯著抑制藥物敏感和藥物抗性多發(fā)性骨髓瘤(MM)細(xì)胞增長（IC50為5–20μM），并通過激活caspases誘導(dǎo)細(xì)胞凋亡。 |
| 體內(nèi)活性 | 在雞胚中，Tubacin抑制HDAC6的活性可以減少在matrigel/尼龍網(wǎng)中新血管的形成。在小鼠體內(nèi)植入的血管生成器中，Tubacin同樣阻礙了新血管的形成。 |
| 存儲條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 93 mg/mL (128.8 mM)
Ethanol : <1 mg/mL
H2O : <1 mg/mL
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| 關(guān)鍵字 | Inhibitor | HDAC | Virus Protease | inhibit | Tubacin | Histone deacetylases |
| 相關(guān)產(chǎn)品 | Valproic acid sodium salt | 4-Phenylbutyric acid | Anthraquinone | Panobinostat | Theophylline | Curcumin | 2-Phenylethanol | Sodium 4-phenylbutyrate | Phenytoin sodium |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗衰老化合物庫 |