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Tubastatin A TFA {[allProObj[0].p_purity_real_show]}

货号:A531870 同义名: TSA TFA; Tubastatin A (trifluoroacetate salt)

Tubastatin A (TSA) TFA是一种高效、选择性的 HDAC6 抑制剂,在无细胞试验中的 IC50 为 15 nM,相对于所有其他同工酶具有 1000 倍的选择性,除 HDAC8 (57 倍)。TSA TFA 还抑制 HDAC10 和金属-β-内酰胺酶结构域蛋白 2 (MBLAC2)。

Tubastatin A TFA 化学结构 CAS号:1239262-52-2
Tubastatin A TFA 化学结构
CAS号:1239262-52-2
Tubastatin A TFA 3D分子结构
CAS号:1239262-52-2
Tubastatin A TFA 化学结构 CAS号:1239262-52-2
Tubastatin A TFA 3D分子结构 CAS号:1239262-52-2
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Tubastatin A TFA 纯度/质量文件 产品仅供科研

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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

95%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
Lys05 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。
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

99%
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

99%
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

97%
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。
产品名称 Capase-7 Caspase Caspase-1 Caspase-10 Caspase-2 Caspase-3 Caspase-4 Caspase-5 Caspase-6 Caspase-8 Caspase-9 其他靶点 纯度
Emricasan 99%+
Z-VAD(OMe)-FMK 99%+
Z-VAD-FMK 99%+
Q-VD-OPh 97%
VX-765 ++++

Caspase-1, Ki: 0.8 nM

++++

Caspase-4, Ki: <0.6 nM

99%+
Ac-DEVD-CHO +++

caspase-7, Ki: 1.6 nM

+++

Caspase-1, Ki: 18 nM

+++

caspase-10, Ki: 12 nM

+

caspase-2, Ki: 1.71 μM

++++

Caspase-3, Ki: 230 pM

++

Caspase-4, Ki: 132 nM

++

caspase-5, Ki: 205 nM

+++

caspase-6, Ki: 31 nM

++++

caspase-8, Ki: 0.92 nM

++

Caspase-9, Ki: 60 nM

98%+
Z-DEVD-FMK 98%
Z-IETD-FMK 98%
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 TFA 生物活性

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]. Treatment of CC12 cells with Tubastatin A results in impaired myotube formation when alpha-tubulin undergoes early hyperacetylation during the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyperacetylated in mature myotubes[3]. A recent study suggests that treatment with Tubastatin A 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

Daily administration of Tubastatin A at a dose of 0.5 mg/kg suppresses HDAC6, 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].

Treatment of CC12 cells with Tubastatin A results in impaired myotube formation when alpha-tubulin undergoes early hyperacetylation during the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyperacetylated in mature myotubes[3].

A recent study suggests that treatment with Tubastatin A 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 TFA 参考文献

[1]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.

[2]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

[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 TFA 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.13mL

2.23mL

1.11mL

22.25mL

4.45mL

2.23mL

Tubastatin A TFA 技术信息

CAS号1239262-52-2
分子式C22H22F3N3O4
分子量 449.42
SMILES Code O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1.O=C(O)C(F)(F)F
MDL No. MFCD24873137
别名 TSA TFA; Tubastatin A (trifluoroacetate salt); Tubastatin A trifluoroacetate salt
运输蓝冰
InChI Key AVAOVICSJJIYRZ-UHFFFAOYSA-N
Pubchem ID 50898504
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

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