Tubacin | HDAC6 Inhibitor | AmBeed-信号通路专用抑制剂

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Tubacin {[allProObj[0].p_purity_real_show]}

货号：A167094

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.

Tubacin 化学结构
CAS号：537049-40-4

Tubacin 3D分子结构
CAS号：537049-40-4

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Tubacin 纯度/质量文件产品仅供科研

货号：A167094 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

组蛋白去乙酰化酶亚型比较

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	EGFR,HER2	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													95%
Panobinostat			++++ HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												Nrf2,NF-κB	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											p53,NF-κB	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			98%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			99+%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tubacin 生物活性

靶点	HDAC6 HDAC6, IC50:4 nM
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]

Tubacin 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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

Tubacin 动物研究

Dose	Mice: min = 25 mg/kg^[9], max = 50 mg/kg^[11]
Administration	i.p.

Tubacin 参考文献

[1]Estiu G, Greenberg E, et al. Structural origin of selectivity in class II-selective histone deacetylase inhibitors. J Med Chem. 2008;51(10):2898-906.

[2]Butler KV, Kalin J, et al. Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A. J Am Chem Soc. 2010;132(31):10842-6.

[3]Wang XX, Wan RZ, Liu ZP. Recent advances in the discovery of potent and selective HDAC6 inhibitors. Eur J Med Chem. 2018.

[4]Haggarty SJ, Koeller KM, et al. Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays. Chem Biol. 2003;10(5):383-96.

[5]Haggarty SJ, Koeller KM, et al. Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation. Proc Natl Acad Sci U S A. 2003;100(8):4389-94.

[6]Tran AD, Marmo TP, et al. HDAC6 deacetylation of tubulin modulates dynamics of cellular adhesions. J Cell Sci. 2007;120(Pt 8):1469-79.

[7]Rao R, Fiskus W, et al. HDAC6 inhibition enhances 17-AAG--mediated abrogation of hsp90 chaperone function in human leukemia cells. Blood. 2008;112(5):1886-93.

[8]Cabrero JR, Serrador JM, et al. Lymphocyte chemotaxis is regulated by histone deacetylase 6, independently of its deacetylase activity. Mol Biol Cell. 2006;17(8):3435-45.

[9]Ota S, Zhou ZQ, Hurlin PJ. Suppression of FGFR3- and MYC-dependent oncogenesis by tubacin: association with HDAC6-dependent and independent activities. Oncotarget. 2018;9(3):3172-3187.

[10]Chan CT, Qi J, et al. Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects. Cancer Res. 2014;74(24):7475-86.

Tubacin 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.93mL

1.39mL

0.69mL

13.85mL

2.77mL

1.39mL

Tubacin 技术信息

CAS号	537049-40-4
分子式	C₄₁H₄₃N₃O₇S
分子量	721.861

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 105 mg/mL(145.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

Tubacin {[allProObj[0].p_purity_real_show]}

Tubacin 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Tubacin 质控信息

Tubacin 生物活性

Tubacin 细胞研究

Tubacin 动物研究

Tubacin 参考文献

Tubacin 实验方案

Tubacin 技术信息

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Tubacin {[allProObj[0].p_purity_real_show]}

Tubacin 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Tubacin 质控信息

Tubacin 生物活性

Tubacin 细胞研究

Tubacin 动物研究

Tubacin 参考文献

Tubacin 实验方案

Tubacin 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Tubacin 纯度/质量文件产品仅供科研