Tubacin
Tubacin 是一种高度有效的选择性的，可逆的，细胞渗透性HDAC6抑制剂，无细胞试验中IC50为4 nM，比作用于HDAC1的选择性高350倍。Tubacin 可通过减少病毒RNA合成来抑制乙型脑炎病毒的复制。
Tubacin Chemical Structure
CAS: 537049-40-4
产品质控
批次：
纯度：
99.19%
99.19
Tubacin相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HeLa | Function assay | 6 hrs | Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay, IC50=2.9μM | 25454270 | |
| A549 | Function assay | 20 hrs | Inhibition of HDAC-6 in human A549 cells assessed as induction of alpha-tubulin acetylation after 20 hrs by cytoblot analysis, EC50=2.5μM | ChEMBL | |
| RAW264.7 | Function assay | Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability | 16408003 | ||
| T24 | Function assay | Induction of histone H3 acetylation in human T24 cells, EC50=2.9μM | 19111466 | ||
| mammalian cells | Function assay | Tested for inhibition of Histone deacetylase 6 induced acetylated tubulin in mammalian cells, EC50=2.9μM | 14584932 | ||
| CHO | Function assay | Inhibition of Bacillus anthracis anthrax protective antigen heptamer pre-pore to pore conversion in CMG2-expressing CHO cells | 23964961 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tubacin 是一种高度有效的选择性的，可逆的，细胞渗透性HDAC6抑制剂，无细胞试验中IC50为4 nM，比作用于HDAC1的选择性高350倍。Tubacin 可通过减少病毒RNA合成来抑制乙型脑炎病毒的复制。 | ||
|---|---|---|---|
| 特性 | 第一个已知的选择性α-微管蛋白脱乙酰基抑制剂。 | ||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在A549细胞中，Tubacin增加α微管蛋白乙酰化，而不直接稳定微管，EC50 是2.5 μM。Tubacin抑制HDAC6介导的α-微管蛋白去乙酰化，并抑制野生型和HDAC6过表细胞的迁移。[2]Tubacin联合使用显著增加微管蛋白乙酰化。[3]Tubacin显著抑制药物敏感和耐药的MM细胞的生长，IC50 是 5–20 μM，并且通过激活caspases诱导细胞凋亡。[4] |
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|---|---|---|---|---|
| 激酶实验 | 酶抑制试验 | |||
| 酶抑制实验通过Reaction Biology HDAC Spectrum平台进行。HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, 和 11的测试用离体重组的人类蛋白，HDAC3/NcoR2 复合体用于HDAC3实验。HDAC1, 2, 3, 6, 10, 和11的底物是来自P53残基379-382 (RHKKAc)的荧光肽；HDAC8的底物是基于p53 (RHKAcKAc)残基379-382的荧光二肽。Acetyl-Lys(三氟乙酰)-AMC作为实验HDAC4, 5, 7,和 9的底物。化合物溶于DMSO，以30 μM为初始浓度，3倍连续稀释，测定10个剂量的IC50。对照化合物Trichostatin A (TSA)初始浓度为5uM，3倍连续稀释，测定10个剂量的IC50。IC50值通过计算剂量反应曲线的斜率得到。 | ||||
| 细胞实验 | 细胞系 | 药物敏感性(MM.1S, U266, INA-6, 和RPMI8226) 和耐药性(RPMI-LR5 和 RPMI-Dox40) MM 细胞系 | ||
| 浓度 | ~20 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 对MM细胞生长的抑制作用通过溴化噻唑蓝四氮唑(MTT)染料吸收值测定。所有实验重复4次。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Acetyl-α-tubulin / α-tubulin / pERK / ERK / p-MLC / MLC |
|
26783207 | |
| Immunofluorescence | p62 / HDAC6 Phalloidin / MYH9 Acetylated Microtubules / Viral HA |
|
26643866 | |
| Growth inhibition assay | Cell viability |
|
29845122 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在鸡胚中，Tubacin抑制HDAC6活性而降低人工基底膜/聚酰胺纤维筛孔中新生血管的形成。在angioreactors移植的小鼠模型中，Tubacin也会损坏新血管形成。[5] |
|
|---|---|---|
| 动物实验 | Animal Models | 植入angioreactors的无胸腺裸鼠 |
| Dosages | -- | |
| Administration | Tubacin填满半闭合的angioreactors, 随后植入小鼠体内。 | |
化学信息&溶解度
| 分子量 | 721.86 | 分子式 | C41H43N3O7S |
| CAS号 | 537049-40-4 | SDF | -- |
| Smiles | C1C(OC(OC1C2=CC=C(C=C2)CO)C3=CC=C(C=C3)NC(=O)CCCCCCC(=O)NO)CSC4=NC(=C(O4)C5=CC=CC=C5)C6=CC=CC=C6 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (138.53 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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