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Tubastatin A HCl

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Chemical Structure| 1310693-92-5 同义名 : TSA HCl;Tubastatin A Hydrochloride
CAS号 : 1310693-92-5
货号 : A107990
分子式 : C20H22ClN3O2
纯度 : 98%
分子量 : 371.861
MDL号 : MFCD20488052
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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

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].
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
实验方案
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
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.