store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tubacin 是一种高效、选择性、可逆、可渗透细胞的 HDAC6 抑制剂,IC50 为 4 nM,选择性是 HDAC1 的约 350 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 652 | 现货 | ||
5 mg | ¥ 1,990 | 现货 | ||
10 mg | ¥ 3,890 | 现货 | ||
25 mg | ¥ 6,250 | 现货 | ||
50 mg | 特惠询价 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,920 | 现货 |
产品描述 | Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1. |
靶点活性 | HDAC6(Cell-free assay):4nM |
体外活性 | 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. Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. 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. |
体内活性 | 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. |
激酶实验 | 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. |
细胞实验 | 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. |
动物实验 | Animal Models: Athymic nude mice implanted with angioreactorsFormulation: DMSODosages: --Administration: Tubacin is filled in semiclosed angioreactors, and then implanted into the mice. |
分子量 | 721.86 |
分子式 | C41H43N3O7S |
CAS No. | 537049-40-4 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (128.8 mM)
Ethanol: <1 mg/mL
H2O: <1 mg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3853 mL | 6.9266 mL | 13.8531 mL | 34.6328 mL |
5 mM | 0.2771 mL | 1.3853 mL | 2.7706 mL | 6.9266 mL | |
10 mM | 0.1385 mL | 0.6927 mL | 1.3853 mL | 3.4633 mL | |
20 mM | 0.0693 mL | 0.3463 mL | 0.6927 mL | 1.7316 mL | |
50 mM | 0.0277 mL | 0.1385 mL | 0.2771 mL | 0.6927 mL | |
100 mM | 0.0139 mL | 0.0693 mL | 0.1385 mL | 0.3463 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tubacin 537049-40-4 Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Virus Protease HDAC Inhibitor inhibit Histone deacetylases inhibitor