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CAS No.: 1252003-15-8

Tubastatin A Catalog No. CSN17162

Synonyms: Tubastatin A

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM and is selective(1000-fold more) against all other isozymes except HDAC8(57-fold more).

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HDAC6

IC50:15nM
描述HDACs (Histone deacetylases) are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs, HDAC 1-11 and sirt 1-7^[2]. Tubastatin A, a derivative from tubacin, is a selective HDAC6 inhibitor with IC50 value of 15nM (measured by purified human HDAC protein), over 1000-fold selectivity against HDAC1. Treatment of Tubastatin A with low concentration (2.5uM) results in an α-tubulin hyperacetylation, corresponding to HDAC6 inhibition, rather than histone hyperacetylation, corresponding to class I HDAC inhibition, which shows the selectivity to HDAC6 of tubastatin A. Tubastatin A possesses the function of modulation of several neurodegenerative diseases. In an HCA oxidative stress assay, tubastatin A displayed neuroprotection against HCA-induced neuronal cell death at 5-10 µM in a dose-dependent manner^[1]. Tubastatin A can also increase autophagic flux and reduce diffuse mutant huntingtin in striatal neurons^[3]. Compared with tubacin, tubastatin A possesses a drug-like property, which makes it more considered as a promising anti-cancer drug^[4]. Combination with tubastatin A can enhance the TMZ-induced cytotoxicity in TMZ-resistant glioma cell lines at concentration < 30 μM^[5].
作用机制Tubastatin has a hydroxamate-based structure, which can chelate the Zn²⁺ ion of HDACs. ^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HeLa cells	-	Function assay	6 h	Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay, IC50=2.5 μM.	25454270
human Jurkat cells	-	Cytotoxic assay	72 h	Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=3.38 μM.	24304348
human KB cells	-	Cytotoxic assay	72 h	Cytotoxicity against human KB cells after 72 hrs by MTS assay, IC50=14.81 μM.	25899338

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动物研究
剂量
Mice^[8] (i.p.): 10 mg/kg - 100 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Mice^[8] (i.p.): 10 mg/kg - 100 mg/kg
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9815 mL
- 14.9076 mL
- 29.8151 mL
- 5 mM
- 0.5963 mL
- 2.9815 mL
- 5.9630 mL
- 10 mM
- 0.2982 mL
- 1.4908 mL
- 2.9815 mL

技术信息

CAS号

1252003-15-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H21N3O2

运输

蓝冰

分子量

335.40

别名

Tubastatin A

溶解度

DMSO	50.0 mg/mL (149.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

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