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生物活性
ITSA-1 is a suppressor of Trichostatin A (TSA) and a molecular tool for dissecting gene regulation by distinct aceytlation events (histone and tubulin). ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC inhibitors. ITSA-1 rreverses TSA induced histone acetylation, overall deacetylation. ITSA-1 also reverses TSA induced cell cycle arrest and apoptosis. Effective range 50 μM.
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体外研究
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体内研究
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激酶实验
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细胞实验
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动物实验
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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 A的Km系数 |
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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。
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参考文献
[1] Koeller KM et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histoneand tubulin acetylation. Chem Biol. 2003 May;10(5):397-410.
[2] Matthew A. McBrian,et al. Histone Acetylation Regulates Intracellular pH. Mol Cell. Author manuscript; available in PMC 2014 Jan 15. Published in final edited form as: Mol Cell. 2013 Jan 24; 49(2): 310–321. Published online 2012 Nov 29. doi: 10.1016/j.molcel.2012.10.025.
[3] Haggarty, S.J., et al. 2003. Chem. Biol. 10: 1267-1279. PMID: 14700634
分子式
C₁₃H₇Cl₂N₃O |
分子量
292.12 |
CAS号
200626-61-5 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
55 mg/mL |
Water
<1 mg/mL |
Ethanol
4 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
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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