Tubastatin A

For research use only. Not for use in humans.

目录号:S8049

Tubastatin A Chemical Structure

CAS No. 1252003-15-8

Tubastatin A 是一种有效的,选择性HDAC6抑制剂,无细胞试验中IC50为15 nM,选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促进自噬并增加凋亡。

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客户使用Selleck生产的Tubastatin A发表文献59篇:

产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Tubastatin A 是一种有效的,选择性HDAC6抑制剂,无细胞试验中IC50为15 nM,选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促进自噬并增加凋亡。
靶点
HDAC6 [1]
(Cell-free assay)
15 nM
体外研究

Tubastatin A选择性作用于所有同工酶除了HDAC8,对所有亚型不含HDAC8,保持超过1000倍的选择性,对HDAC8具有约57倍的选择性。2.5 μM Tubastatin A优先诱导α-tubulin 高度乙酰化。10 μM Tubastatin A轻微诱导组蛋白乙酰化。Tubastatin A 5 μM开始对同型半胱氨酸诱导的神经元细胞死亡具有保护作用,这种作用具有剂量依赖性,10 μM时,达到完全保护。[1]Tubastatin A (10 μM) 作用于胆管癌细胞系,诱导乙酰化的α-tubulin水平增加,和初级纤毛表达的恢复,初级纤毛表达的恢复与下调Hedgehog (Hh)和MAPK信号通路,以及减少细胞增殖率(平均50%)和浸润(40%)相关。[2]Tubastatin A作用于LPS刺激的人类 THP-1巨噬细胞,显著抑制TNF-α和IL-6,IC50分别为272 nM 和 712 nM。Tubastatin A作用于小鼠Raw 264.7巨噬细胞,抑制一氧化氮(NO)分泌,这种作用具有剂量依赖性,IC50为4.2 μM。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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PC12 NEHLR2FCdnSrb4jp[IFvfCCjc4PhfS=> NVHhRWZiPSC3TR?= NWWwWGl5OjRiaILz M4DO[2FvfGmxeHnkZY51KGGldHn2bZR6KGGpYXnud5QhUDKRMj3pcoR2[2WmIH;4bYRifGm4ZTDzeJJme3NiaX6gdoF1KFCFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hWk:VIHHjZ5VufWyjdHnvckBifCB3IIXNJJBz\WmwY4XiZZRm\CCob4KgNlQhcHK|IH\vcIxwf2WmIHL5JGgzVzJiY3jhcIxmdmenIHHu[EBu\WG|dYLl[EBi\nSncjCxNkBpenNiY3;pcoN2[mG2ZXSge4l1cCCnYoPlcIVvKGK7IFTDSmguTEFiZInlMYJie2WmIH\seY9z\Q>? NFHGVZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO4OVIzPyd-M{CzPFUzOjd:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
EGFR / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29665050     


In KYSE140 (C) and KYSE180 (D), Tubastatin treatment EGFR, AKT, phosphoAKT and phospho-ERK levels were decreased in tubastatin-treated cells compared with control group.

29665050
Immunofluorescence
α-tubulin / Acetylated tubulin ; 

PubMed: 23798680     


Effects of tubastatin A on microtubules and microtubule acetylation level are shown. MCF-7 cells were treated with different concentrations of tubastatin A for 24 h and processed for immunostaining with antibodies against α-tubulin (green) and acetylated tubulin (red). Scale bars, 10 μm.

HDAC6; 

PubMed: 23798680     


MCF-7 cells are treated with vehicle, 30 μM tubastatin A (TBA), or 240 nM TSA for 24 h and fixed and processed to visualize microtubules (red) and HDAC6 (green). Scale bar, 20 μm.

23798680
体内研究 Tubastatin A降低体内胆管癌的生长。Tubastatin A(10 mg/kg)处理同基因大鼠原位胆管癌模型,诱导低于平均瘤重6倍,降低肿瘤重量与肝脏重量和体重(分别为5和5.6倍)的比值。Tubastatin A 处理肿瘤,与对照组相比,显著降低PCNA阳性细胞的量(34% vs 65%)。[2]Tubastat A按30 mg/kg剂量腹腔注射给药弗氏完全佐剂(FCA)诱导的动物炎症模型,显著抑制鼠爪体积。Tubastat A(30 mg/kg 腹腔注射)处理胶原诱导型关节炎DBA1小鼠的爪子组织,显著降低临床评分(〜70%),和IL-6表达。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[4]

- 合并

HDAC酶试验:

Tubastatin A在实验 Buffer(50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA,和 20 μM tris(2-carboxyethyl)phosphine) 中溶解和稀释到终浓度的6倍。HDAC酶在实验 Buffer 中稀释到终浓度的1.5倍,与Tubastatin A预温育10分钟,然后加入底物。 通过滴定曲线测得,用于每种酶的FTS(HDAC1, HDAC2, HDAC3, 和HDAC6) 或 MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, 和 HDAC9)量等于米氏常数(Km)。使用0.3 μM测序级胰蛋白酶将FTS或MAZ-1675在实验 Buffer中稀释到终浓度的6倍。底物/胰蛋白酶混合物加入到酶/化合物混合物中,震荡实验板60秒,然后置于SpectraMax M5酶标仪上。赖氨酸侧链在肽底物中脱乙酰化后,监测酶促反应的7-amino-4-methoxy-coumarin释放,监测30分钟,计算反应的线性速率。
细胞实验:

[2]

- 合并
  • Cell lines: 人体胆管癌细胞系HuCCT-1
  • Concentrations: ~10 μM
  • Incubation Time: 21 天
  • Method:

    细胞生长在软琼脂中,测评锚定非依赖性生长。约25,000个细胞悬浮在培养基的0.4%琼脂中,超过1%琼脂层在6孔板中。每周加入两次培养基,温育21天,拍摄图片。使用Gel-Pro软件分析菌落的数量和尺寸。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 携带胆管癌移植瘤BDEneu的大鼠
  • Dosages: 10 mg/kg
  • Administration: 每天腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 67 mg/mL warmed (199.76 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG 300+5%Tween 80+50% ddH2O
1.67mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 335.4
化学式

C20H21N3O2

CAS号 1252003-15-8
储存条件 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    We are planning to order some tubastatin A but I found out there are two versions of it. One has HCl and one does not. Which one do you recommend for live cell use? Will the HCl containing version significantly change the pH?

  • 回答:

    S8049 and S2627 have same molecular structure. The only difference is S2627 containing HCl and has higher solubility in DMSO (74 mg/mL vs. S8049 9 mg/mL). Since they are the same molecule, the biological function should be similar. I would recommend to use S2627 for cell culture study.

  • 问题 2:

    What’s the vehicle do you recommend to dissolve the compound for in vivo experiments?

  • 回答:

    S8049 Tubastatin A can be dissolved in 2% DMSO/30% PEG 300/PBS at 2.5 mg/mL as a clear solution, and it is also a clear solution in 2% DMSO/ corn oil at 2.5 mg/mL. The drug in 2% DMSO/0.5% Tween 80/PBS is a homogeneous suspension at 2.5 mg/mL at first. After stay for a while, the precipitation goes out at the bottom of the tube.

HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID