产品说明书

Trichostatin A

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Chemical Structure| 58880-19-6 同义名 : 曲古柳菌素A ;TSA
CAS号 : 58880-19-6
货号 : A725112
分子式 : C17H22N2O3
纯度 : 99%+
分子量 : 302.37
MDL号 : MFCD03848392
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: 50 mg/mL(165.36 mM)，配合低频超声助溶，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
动物实验配方：

2% DMSO+30% PEG 300+2% Tween 80+water 1.5 mg/mL

生物活性
靶点

  • HDAC

    HDAC, IC50:~1.8 nM
描述 HDACs are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs divided into four classes: class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10), class III (sirtuin family: sirt1-sirt7) and class IV (HDAC11)[1]. Trichostatin A (TSA) is the inhibitors of the class I and class II HDACs with IC50 value of 2.4 ± 0.5 nM (measured by HDAC activity in cellular extracts). Trichostatin A treatment with concentration of 2 μM for 24h can increase histone H4 hyperacetylation in all of the breast cancer cell lines tested (MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3) significantly and inhibit the cell growth with IC50 values ranging in 26 – 308 nM in 96h. Treatment of 500 μg/kg trichostatin A by s.c injection daily for 4 weeks significantly inhibited tumor growth in Ludwig/Wistar/Olac female rats bearing tumors induced with NMU, compared with control[2]. Trichostatin A is usually used in the study of tumor growth inhibition. The cell death and cell cycle arrest induced by it may involve in several mechanisms including transcription-dependence and -independence, such as cell cycle arrest, apoptosis, the regulation of ROS and the inhibition of angiogenesis[3].
作用机制 Trichostatin A comprises a hydroxamic acid-based metal-binding domain that coordinates the catalytic Zn(II) in the HDAC active site[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
A2780 0.05-2 μM Growth Inhibition Assay 10/24/48 h mediates growth arrest in a concentration- and time-dependent manner 24223801
A431 2/10/50/100nM Apoptosis Assay 48h inhibits the cell growth 25371069
A431 50nM Function Assay 2/6/12/24h activates p21 and inhibits ATF3 expression 25371069
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03049124 Rectal Cancer Not Applicable Recruiting July 31, 2019 Canada, Ontario ... 展开 >> University of Ottawa Recruiting Ottawa, Ontario, Canada, K1N 6N5 Contact: Amanda Wurz, MSc    613-562-5800 ext 3626    amanda.wurz@uottawa.ca 收起 <<
NCT02152267 Craniomandibular Disorders Not Applicable Completed - Brazil ... 展开 >> Federal University of Bahia Salvador, Bahia, Brazil, 40110-902 收起 <<
NCT01028014 Urethral Sphincter Activity Not Applicable Completed - United States, Alabama ... 展开 >> University of Alabama at Birmingham, The Kirklin Clinic Birmingham, Alabama, United States, 35233 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.54mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL
参考文献

[1]Yoon S, Eom GH, et al. HDAC and HDAC Inhibitor: From Cancer to Cardiovascular Diseases. Chonnam Med J. 2016 Jan;52(1):1-11.

[2]Vigushin DM, Ali S, et al. Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo. Clin Cancer Res. 2001 Apr;7(4):971-6.

[3]Xu WS, Parmigiani RB, et al. Histone deacetylase inhibitors: molecular mechanisms of action. Oncogene. 2007 Aug 13;26(37):5541-52.

[4]Codd R, Braich N, et al. Zn(II)-dependent histone deacetylase inhibitors: suberoylanilide hydroxamic acid and trichostatin A. Int J Biochem Cell Biol. 2009 Apr;41(4):736-9.

[5]Sanderson L, Taylor GW, et al. Plasma pharmacokinetics and metabolism of the histone deacetylase inhibitor trichostatin a after intraperitoneal administration to mice. Drug Metab Dispos. 2004 Oct;32(10):1132-8. Epub 2004 Jul 21.