Tubastatin A HCl | TSA HCl | HDAC6 Inhibitor | AmBeed-信号通路专用抑制剂

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Tubastatin A盐酸盐 /Tubastatin A HCl {[allProObj[0].p_purity_real_show]}

货号：A107990 同义名： TSA HCl;Tubastatin A Hydrochloride

Tubastatin A HCl是一种强效和选择性的 HDAC6 抑制剂，在无细胞测定中 IC50 为 15 nM。它对所有其他同工酶的选择性高 1000 倍，除了 HDAC8，它对其的选择性高 57 倍。Tubastatin A HCl还抑制 HDAC10 和含金属 β-内酰胺酶结构域蛋白 2 (MBLAC2)。

Tubastatin A HCl 化学结构
CAS号：1310693-92-5

Tubastatin A HCl 3D分子结构
CAS号：1310693-92-5

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Tubastatin A HCl 纯度/质量文件产品仅供科研

货号：A107990 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	HER2,EGFR	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													95%
Panobinostat			++++ HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												NF-κB,Nrf2	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				✔											NF-κB,p53	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。

Tubastatin A HCl 生物活性

靶点	HDAC8 HDAC8, IC50:854 nM HDAC6 HDAC6, IC50:15 nM
描述	Tubastatin A exhibits significant selectivity towards all 11 HDAC isoforms, maintaining over 1000-fold selectivity against all isoforms except HDAC8, for which it demonstrates approximately 57-fold selectivity. In assays assessing homocysteic acid (HCA)-induced neurodegeneration, Tubastatin A demonstrates dose-dependent protection against HCA-induced neuronal cell death, with significant protection observed at 5 μM and near complete protection at 10 μM^[1]. Tubastatin A at a concentration of 100 ng/mL enhances the suppressive effect of Foxp3⁺ T-regulatory cells (Tregs) on T cell proliferation in vitro^[2]. In CC12 cells, Tubastatin A treatment results in impaired myotube formation when alpha-tubulin undergoes early hyperacetylation during the myogenic process; however, myotube elongation ensues when alpha-tubulin is hyperacetylated in mature myotubes^[3]. Tubastatin A treatment enhances cell elasticity, as demonstrated by atomic force microscopy (AFM) tests, without causing significant alterations to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L^[4].
体内研究	Administering Tubastatin A daily at a dosage of 0.5 mg/kg suppresses HDAC6 activity, thereby enhancing the suppressive function of Tregs in mouse models of inflammation and autoimmunity, including various experimental colitis models and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection^[2].
体外研究	Tubastatin A exhibits significant selectivity towards all 11 HDAC isoforms, maintaining over 1000-fold selectivity against all isoforms except HDAC8, for which it demonstrates approximately 57-fold selectivity. In assays assessing homocysteic acid (HCA)-induced neurodegeneration, Tubastatin A demonstrates dose-dependent protection against HCA-induced neuronal cell death, with significant protection observed at 5 μM and near complete protection at 10 μM^[1]. Tubastatin A at a concentration of 100 ng/mL enhances the suppressive effect of Foxp3⁺ T-regulatory cells (Tregs) on T cell proliferation in vitro^[2]. In CC12 cells, Tubastatin A treatment results in impaired myotube formation when alpha-tubulin undergoes early hyperacetylation during the myogenic process; however, myotube elongation ensues when alpha-tubulin is hyperacetylated in mature myotubes^[3]. Tubastatin A treatment enhances cell elasticity, as demonstrated by atomic force microscopy (AFM) tests, without causing significant alterations to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L^[4].

Tubastatin A HCl 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
134/04	7.5 µM	Function assay		impairs myotube formation	22174839
293T	~2 μg/ml	Function assay		induces PTEN expression and membrane translocation	26279303
293T	~2 μg/ml	Function assay		induces PTEN acetylation at K163	26279303
C2C12	7.5 µM	Function assay		impairs myotube formation	22174839

Tubastatin A HCl 参考文献

[1]Kyle V. Butler et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A J. Am. Chem. Soc., 2010, 132 (31), pp 10842-10846

[2]de Zoeten EF, et al. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May;31(10):2066-78.

[3]Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563

[4]Ketene AN, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells. Integr Biol (Camb). 2012 May;4(5):540-9.

Tubastatin A HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.45mL

2.69mL

1.34mL

26.89mL

5.38mL

2.69mL

Tubastatin A HCl 技术信息

CAS号	1310693-92-5
分子式	C₂₀H₂₂ClN₃O₂
分子量	371.861

别名	TSA HCl;Tubastatin A Hydrochloride
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 10 mg/mL(26.89 mM)，配合低频超声，并水浴加热至45℃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

H₂O: 6.5 mg/mL(17.48 mM)，配合低频超声助溶

动物实验配方

5%DMSO+40%PEG300+5%Tween80+50%water 5.5 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

134/04	7.5 µM	Function assay	impairs myotube formation	22174839
293T	~2 μg/ml	Function assay	induces PTEN expression and membrane translocation	26279303
293T	~2 μg/ml	Function assay	induces PTEN acetylation at K163	26279303
C2C12	7.5 µM	Function assay	impairs myotube formation	22174839
CaSki	~5 μM	Function assay	induces the differential α-tubulin acetylation	23698468
CaSki	~5 μM	Function assay	inhibits Thapsigargin- or EGF-induced SOCE activation	23698468
CML-T1	10 μM	Function assay	enhances cell adhesivity to fibronectin	23022583
HaCaT keratinocytes	10 μM	Function assay	blocks arsenite from inducing Nrf2 protein translation	22367689
HEK293T	~3 μM	Function assay	up-regulated XBP1s protein level	24909686
HEK293T	~3 μM	Function assay	delays XBP1s protein degradation via acetylation-mediated proteasomal degradation	24909686
HL-60	10 μM	Function assay	enhances cell adhesivity to fibronectin	23022583
HT3	~5 μM	Function assay	induces the differential α-tubulin acetylation	23698468
Huh7	~5 μM	Function assay	suppresses proliferation of hepatitis C virus replicon with EC50 = 0.3 μM	25108326
IPC298	~3 μM	Function assay	augments expression of MHC class I and melanoma associated antigens	25957812
JURL-MK1	10 μM	Function assay	enhances cell adhesivity to fibronectin	23022583
K562	10 μM	Function assay	enhances cell adhesivity to fibronectin	23022583
KMCH	~10 μM	Growth inhibitory assay	decreases proliferation and anchorage-independent growth	23370327
MCF-7	30 μM	Growth inhibitory assay	IC50=15 μM	23798680
MCF-7	30 μM	Function assay	increases the microtubule acetylation level.	23798680
MCF-7	30 μM	Function assay	stabilizes microtubules against cold-induced depolymerization	23798680
MCF-7	15 μM	Function assay	stabilizes microtubules against nocodazole-induced disassembly	23798680
MCF-7	30 μM	Function assay	alteres the assembly dynamics of interphase microtubules	23798680
MCF-7	30 μM	Function assay	increases the binding of HDAC6 with interphase microtubules	23798680
neuron cultures	2.5 μM	Kinase assay	induces α-tubulin hyperacetylation	20614936
neuron cultures	~10 μM	Function assay	protects against glutathione depletion-induced oxidative stress	20614936
PC12	~3 μM	Function assay	up-regulates anti-oxidative gene expression related to transcription factor XBP1s	24909686
PC12	~3 μM	Growth inhibitory assay	reverse H2O2-induced growth inhibition	24909686
RAW 264.7	~10 μM	Function assay	attenuates NO production	23541634
SACC-83	~2 μg/ml	Function assay	induces PTEN expression and membrane translocation	26279303
SiHa	~5 μM	Function assay	induces the differential α-tubulin acetylation	23698468
SiHa	~5 μM	Function assay	inhibits Thapsigargin- or EGF-induced SOCE activation	23698468
SKMEL103	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
SKMEL21	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
SKMEL28	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
SKMEL30	~3 μM	Function assay	augments expression of MHC class I and melanoma associated antigens	25957812
TCa83		Function assay	induces PTEN expression and membrane translocation	26279303
THP-1	~10 μM	Function assay	inhibits TNF-α and IL-6 secretion	23541634
U-87 MG	~2 μg/ml	Function assay	inhibits the migration and invasion	26279303
U-87 MG	~10 μM	Function assay	inhibits AKT phosphorylation	26279303
U-87 MG	~10 μM	Growth inhibitory assay	inhibits cell growth	26279303
WM1361a	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
WM1366	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
WM164	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
WM164	~6 μM	Function assay	induce G1 arrest	25957812
WM164	~3 μM	Function assay	augments expression of MHC class I and melanoma associated antigens	25957812
WM35	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
WM793	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
WM793	~6 μM	Function assay	induce G1 arrest	25957812
WM983a	~500 nM	Growth inhibitory assay	inhibits cell proliferation	25957812
WM983a	~6 μM	Function assay	induce G1 arrest	25957812
WM983a	~3 μM	Function assay	augments expression of MHC class I and melanoma associated antigens	25957812

Tubastatin A盐酸盐 /Tubastatin A HCl {[allProObj[0].p_purity_real_show]}

Tubastatin A HCl 纯度/质量文件产品仅供科研

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