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CAS No.: 537049-40-4

Tubacin Catalog No. CSN16346

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1.

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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

IC50:4nM
描述There are 18 mammalian HDACs, HDAC 1-11 and sirt 1-7. One of the member, HDAC6 can target specific substrates like HSP90 and α-tubulin which involve in protein trafficking and degradation or cell shape and migration, thus participates in the pathways relating to neurodegenerative diseases, cancer and immunology^[3]. Tubacin has a high affinity to HDAC6 (Ki=142nM)^[1] and inhibits HDAC6 potently and selectively with an IC50 value of 4nM (measured by purified human HDAC protein), approximately 350-fold selectivity over HDAC1^[2]. Treatment with 2uM tubacin can strongly and selectively increase acetylation level of α-tubulin, corresponding to HDAC6 inhibition, in A549 cells after 19h, with no effect on histone acetylation^[4]. Unlike Taxol, which increases α-tubulin acetylation by direct stabilization of microtubules, tubacin do not directly stabilize microtubules and has no overall effect on the morphology of A549 cells, yet with no effect on gene expression or cell-cycle progression, but it inhibits the migration of cells under normal culture conditions with concentration of 2uM, which may due to the inhibition of HDAC6's functional role as a MAP or capacity to mediate the focal adhesion dynamics required for rapid cell migration^[5]^[6]. Co-treatment with 17-AAG and tubacin can significantly augment the loss of survival of K562 cells and viability of AML and CML samples, which suggests that HDAC6 is an hsp90 client protein and can augment the anti-leukemia effects of 17-AAG^[7].
作用机制Tubacin inhibitd the HDAC6 by chelating a Zn++ ion through its hydroxamate structure and appears to alter the formation of complexes of HDAC6.^[5]^[8]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A549 cells	-	Function assay	-	Inhibition of HDAC6 in human A549 cells assessed as induction of alpha-tubulin acetylation by fluorescence microscopy, EC50=2.9 μM	16408003
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=2.9 μM	25454270
human T24 cells	-	Function assay	-	Induction of histone H3 acetylation in human T24 cells, EC50=2.9 μM	19111466

动物研究
剂量
Mice: min = 25 mg/kg^[9], max = 50 mg/kg^[11]

给药途径
i.p.
参考文献

动物研究
剂量	Mice: min = 25 mg/kg^[9], max = 50 mg/kg^[11]
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
- 1.3853 mL
- 6.9266 mL
- 13.8531 mL
- 5 mM
- 0.2771 mL
- 1.3853 mL
- 2.7706 mL
- 10 mM
- 0.1385 mL
- 0.6927 mL
- 1.3853 mL

技术信息

CAS号

537049-40-4

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

C41H43N3O7S

运输

蓝冰

分子量

721.86

别名

溶解度

DMSO	90.0 mg/mL (124.7 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

10 mg/mL

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Tubacin Catalog No. CSN16346

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