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Trichostatin A

曲古柳菌素A,TSA

Trichostatin A (TSA)是一种HDAC抑制剂,IC50为1.8 nM左右,HDAC8是HDAC家族中唯一不受TSA影响的成员。

目录号
EY1563
EY1563
EY1563
纯度
99.61%
99.61%
99.61%
规格
2 mg
5 mg
10 mg
原价
1063
2245
3680
售价
1063
2245
3680
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Trichostatin A简称TSA,是一种常用的HDAC(histone deacetylase)抑制剂。Trichostatin A可以通透细胞,选择性抑制HDACs,但不抑制NAD依赖的SIRT系列的deacetylases。Trichostatin A抑制HDAC后可以导致histone乙酰化水平升高,一些基因的转录水平提高;也可以升高其它一些蛋白的乙酰化水平改变其活力或稳定性。Trichostatin A处理细胞后可以导致细胞周期抑制,目前被看作是一种潜在的抗癌药物。

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~5 mg/kg/day 皮下注射

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Vigushin DM, et al. Clin Cancer Res, 2001, 7(4), 971-976.
    [2] Futamura, M., et al., 1995. Trichostatin A inhibits both ras-induced neurite outgrowth of PC12 cells and morphological transformation of NIH3T3 cells. Oncogene. 10(6): 1119-23.
    [3] Van Lint, C., et al., 1996. Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation. The EMBO journal. 15(5): 1112-20.
    [4] Kawamura, Teruhisa., et al., 2005. Acetylation of GATA-4 is involved in the differentiation of embryonic stem cells into cardiac myocytes. The Journal of biological chemistry. 280(20): 19682-8.
    [5] Takahashi, I., et al., 1996. Selective inhibition of IL-2 gene expression by trichostatin A, a potent inhibitor of mammalian histone deacetylase. The Journal of antibiotics. 49(5): 453-7.
    [6] Pan, Lina., et al., 2007. Histone deacetylase inhibitor trichostatin a potentiates doxorubicin-induced apoptosis by up-regulating PTEN expression. Cancer. 109(8): 1676-88.

    分子式
    C17H22N2O3
    分子量
    302.37
    CAS号
    58880-19-6
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 mg/mL
    Water
    <1 mg/mL
    Ethanol
    1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    Rank NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    1 NCT00876447 Overactive Bladder Biological: Botulinum Toxin Type A 300U|Biological: Botulinum Toxin Type A 200U Allergan Phase 3 2009-01-01 2014-06-12
    2 NCT01157000 Healthy Drug: Canagliflozin Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2010-05-01 2014-04-07
    4 NCT01901198 Healthy Volunteers Biological: Human Serum Albumin/interferon alpha2a 300-1200 mcg single dose S.C.|Biological: Peginterferon 180 mcg single dose S.C. Beijing Bio-Fortune Ltd. Phase 1 2013-04-01 2014-11-14
    5 NCT00834912 Healthy Drug: Tramadol hydrochloride|Drug: Tramadol HCl|Drug: Tramadol HCl Labopharm Inc. Phase 1 2006-02-01 2012-04-25
    6 NCT03066401 Dysmetabolic Syndrome|Hyperferritinemia|Obese Procedure: echography University Hospital, Lille 2015-01-01 2017-02-27
    7 NCT03066414 Genetic Hemochromatosis Procedure: echography University Hospital, Lille 2015-02-01 2017-02-27
    8 NCT01703494 Clostridium Difficile Biological: Fecal Microbiota Transplantation|Biological: Sham Fecal Microbiota Transplantation Colleen Kelly|The Miriam Hospital Phase 2 2012-10-01 2015-09-29
    9 NCT00821834 Stable Angina|Myocardial Infarction Drug: clopidogrel (SR25990)|Drug: ticlopidine|Drug: Placebo Sanofi Phase 3 2008-12-01 2011-07-25
    10 NCT00284518 Benign Prostatic Hyperplasia Biological: botulinum toxin Type A|Drug: normal saline Allergan Phase 2 2005-12-01 2012-11-16
    11 NCT00276198 Iron Deficiency Anemia|Infectious Diseases|Undernutrition Dietary Supplement: Sprinkles|Dietary Supplement: Ferripel-3, Vitamins A&D drops Soroka University Medical Center Phase 3 2005-07-01 2008-04-15
    13 NCT01575054 Muscle Spasticity Biological: botulinum toxin Type A|Drug: Normal Saline Allergan Phase 3 2012-05-01 2016-08-22
    14 NCT01664702 Childhood Obesity Dietary Supplement: Dairy Products|Dietary Supplement: Dairy Servings University of Kansas|Dairy Management Inc. 2005-01-01 2012-08-13
    15 NCT00559260 Sedation for Non-Emergent Upper and/or Lower Endoscopy Device: Passive monitoring with pulse-oximetry, NIBP and ECG Ethicon Endo-Surgery 2003-01-01 2008-09-12
    16 NCT00631345 Prediabetes|Obesity Behavioral: Group-Based Lifestyle Intervention (Phases 1 and 2)|Other: Individual Education Program (All Phases)|Behavioral: Self-Directed Maintenance (Phase 3)|Behavioral: Extended Group Maintenance (Phase 3) Wake Forest University Health Sciences|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) 2007-08-01 2017-03-07
    17 NCT02910635 Abnormalities, Cardiovascular Drug: Volanesorsen|Drug: Moxifloxacin|Drug: Placebo Ionis Pharmaceuticals, Inc.|Akcea Therapeutics Phase 1 2016-09-19 2017-03-07
    18 NCT01869465 Schistosomiasis Other: Pre-treatment snack|Behavioral: Education arm Makerere University|University of Copenhagen 2012-10-01 2013-06-01
    19 NCT01080612 Healthy Drug: 330 mg pregabalin controlled release|Drug: 330 mg pregabalin controlled release|Drug: 330 mg pregabalin controlled release|Drug: 300 mg pregabalin immediate release Pfizer Phase 1 2010-04-01 2015-03-04
    20 NCT02098174 Glomerular Filtration Rate|Acute Kidney Injury Drug: MP-3180|Other: Iohexol comparator MediBeacon Phase 1 2013-11-01 2016-09-21
    21 NCT00439140 Overactive Bladder Biological: botulinum toxin Type A|Drug: Normal Saline (Placebo) Allergan Phase 3 2007-06-01 2013-12-09
    22 NCT00882739 Acute Myocardial Infarction Drug: Clopidogrel 300 mg|Drug: Clopidogrel 600 mg|Drug: Clopidogrel 900 mg Ospedale San Donato Phase 4 2009-04-01 2012-01-25

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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