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Tubacin

Tubacin

产品编号 T6327   CAS 537049-40-4

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。

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Tubacin Chemical Structure
Tubacin, CAS 537049-40-4
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
产品目录号及名称: Tubacin (T6327)
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特惠询价: Tubacin (T6327)
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选择批次  
纯度: 98.71%
纯度: 97.62%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 93 mg/mL (128.8 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Butler KV, et al. J Am Chem Soc. 2010, 132(31), 10842-0846. 2. Haggarty SJ, et al. Proc Natl Acad Sci U S A. 2003, 100(8), 4389-4394. 3. Marcus AI, et al. Cancer Res. 2005, 65(9), 3883-3893. 4. Hideshima T, et al. Proc Natl Acad Sci U S A. 2005, 102(24), 8567-8572. 5. Li D, et al. Protein Cell. 2011, 2(2), 150-160. 6. Lu CY, et al. Tubacin, an HDAC6 Selective Inhibitor, Reduces the Replication of the Japanese Encephalitis Virus via the Decrease of Viral RNA Synthesis. Int J Mol Sci. 2017 May 1;18(5).

文献引用

1. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.
HDAC6-IN-8 HDAC-IN-53 BRD2492 JPS014 TFA CAY10603 RG2833 Rac-Belinostat Suprastat

相关化合物库

该产品包含在如下化合物库中:
染色质修饰分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

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。

Keywords

Tubacin 537049-40-4 Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Virus Protease HDAC Inhibitor inhibit Histone deacetylases inhibitor

 

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