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Tubastatin A Hydrochloride

Tubastatin A Hydrochloride

产品编号 T6161   CAS 1310693-92-5
别名: TSA HCl, Tubastatin A HCl

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。

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Tubastatin A Hydrochloride Chemical Structure
Tubastatin A Hydrochloride, CAS 1310693-92-5
规格 价格/CNY 货期 数量
5 mg ¥ 339 现货
10 mg ¥ 551 现货
50 mg ¥ 677 现货
100 mg ¥ 1,192 现货
200 mg ¥ 1,995 现货
1 mL * 10 mM (in DMSO) ¥ 415 现货
其他形式的 Tubastatin A Hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Tubastatin A Hydrochloride (T6161)
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选择批次  
纯度: 99.25%
纯度: 97.55%
纯度: 97.24%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tubastatin A Hydrochloride (TSA HCl) is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).
靶点活性 HDAC6:15 nM
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]
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]
激酶实验 Enzyme Inhibition Assays: Enzyme inhibition assays are performed by the Reaction Biology Corporation, Malvern, PA, using the Reaction Biology HDAC Spectrum platform. (www.reactionbiology.com) The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays use isolated recombinant human protein; HDAC3/NcoR2 complex is used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10, and 11 assays is a fluorogenic peptide from p53 residues 379-382 (RHKKAc); substrate for HDAC8 is fluorogenic diacyl peptide based on residues 379-382 of p53 (RHKAcKAc). Acetyl-Lys (trifluoroacetyl)-AMC substrate is used for HDAC4, 5, 7, and 9 assays. Tubastatin A is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A (TSA) is tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values are extracted by curve-fitting the dose/response slopes.
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)
别名 TSA HCl, Tubastatin A HCl
分子量 371.86
分子式 C20H21N3O2·HCl
CAS No. 1310693-92-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 3.7 mg/mL (10 mM), Heating is recommended.

H2O: 7.43 mg/mL (20 mM), Sonication and heating are recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.6892 mL 13.4459 mL 26.8918 mL 67.2296 mL
5 mM 0.5378 mL 2.6892 mL 5.3784 mL 13.4459 mL
10 mM 0.2689 mL 1.3446 mL 2.6892 mL 6.723 mL
H2O 20 mM 0.1345 mL 0.6723 mL 1.3446 mL 3.3615 mL

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TargetMol Library Books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.

TargetMol Library Books文献引用

1. Liu S, Zhang H L, Li J, et al.Tubastatin A potently inhibits GPX4 activity to potentiate cancer radiotherapy through boosting ferroptosis.Redox Biology.2023: 102677.
Mycophenolate Mofetil Ac-IETD-CHO TFA PEAQX tetrasodium hydrate Triparanol (S)-(+)-Rolipram Irbesartan Pomalidomide TCS-PIM-1-4a

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 细胞重编程化合物库 染色质修饰分子库 抗胰腺癌化合物库 癌细胞分化化合物库 DNA 损伤和修复分子库 已知活性化合物库 经典已知活性库 抗衰老化合物库 细胞凋亡化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tubastatin A Hydrochloride 1310693-92-5 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Tubastatin A Histone deacetylases Inhibitor inhibit TSA HCl Tubastatin A HCl inhibitor

 

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