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Tubastatin A Hydrochloride

Tubastatin A Hydrochloride (TSA HCl) 是一种选择性的 HDAC6抑制剂，IC50值为 15 nM，对其选择性是 HDAC8 外的其他亚型的 1000 多倍。

CAS号

1310693-92-5

分子式

C20H21N3O2·HCl

主要靶点

Autophagy|Apoptosis|HDAC

仅限科研使用

Cat No : CM04441

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Synonyms

TSA HCl|Tubastatin A HCl

验证数据展示

  • CAS No.: 1310693-92-5

    Tubastatin A Hydrochloride
    CAS#: 1310693-92-5

产品信息

Tubastatin A HCl is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).

CAS号 1310693-92-5
分子式 C20H21N3O2·HCl
主要靶点 Autophagy|Apoptosis|HDAC
主要通路 凋亡|DNA损伤和修复|自噬|表观遗传
分子量 371.86
纯度 99.25%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 TSA HCl|Tubastatin A HCl

靶点活性

HDAC6:15 nM

体内活性

Daily treatment of 0.5 mg/kg Tubastatin A inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, which including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection. [2]

体外活性

Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. [1] Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation at 100 ng/mL in vitro. [2] Tubastatin A treatment in C2C12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes. [3] A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L. [4]

溶解度

DMSO:3.7 mg/mL (10 mM),with gentle warming

细胞实验

Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments are initiated 24 hours after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells are rinsed with warm PBS and then placed in minimum essential medium (Invitrogen) containing 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress is induced by the addition of the glutamate analogue homocysteate (HCA; 5 mM) to the media. HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. In combination with HCA, neurons are treated with Tubastatin A at the indicated concentrations. Viability is assessed after 24 hours by MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method.(Only for Reference)

参考文献

1.Butler KV, et al, J Am Chem Soc, 2010, 132(31), 10842-10846.
2.de Zoeten EF, et al, Mol Cell Biol, 2011, 31(10), 2066-2078.
3.Di Fulvio S, et al, PloS One, 2011, 6(12):e28563.
4.Ketene AN, et al, Integr Biol (Camb), 2012, 4(5), 540-549.

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