Apicidin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Apicidin，一种天然真菌代谢物，是HDAC的选择性抑制剂。
组蛋白去乙酰酶（HDAC）移除组蛋白ε-N-乙酰赖氨酸的乙酰基。据悉，通过对组蛋白赖氨酸残基的可逆性乙酰化作用，组蛋白乙酰转移酶和组蛋白去乙酰化酶在转录激活或抑制基因表达方面起着重要的作用。
Apicidin对顶复门寄生虫具有强效而广泛的活性[1]。实验还表明，它在人类和小鼠肿瘤细胞株中具有强效的抗血管生成活性以及降低HIF-1α的水平[2]。
Apicidin也被广泛地用于体内研究，以明确HDAC在不同生理过程中的作用。Apicidin对小鼠中的不同癌细胞系显现出抗增殖活性[3]。在人结肠癌HCT-116异种移植肿瘤模型中，Apicidin抑制肿瘤生长[4]。同时，它在Ishikawa细胞异种移植肿瘤模型中也显现出抗肿瘤活性[5]。
参考文献：
1. Darkin-Rattray SJ, Gurnett AM, Myers RW, Dulski PM, Crumley TM, Allocco JJ, et al. Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase. Proc Natl Acad Sci U S A 1996, 93:13143-13147.
2. Kim SH, Jeong JW, Park JA, Lee JW, Seo JH, Jung BK, et al. Regulation of the HIF-1alpha stability by histone deacetylases. Oncol Rep 2007, 17:647-651.
3. Han JW, Ahn SH, Park SH, Wang SY, Bae GU, Seo DW, et al. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Res 2000, 60:6068-6074.
4. Jones P, Altamura S, De Francesco R, Paz OG, Kinzel O, Mesiti G, et al. A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo. J Med Chem 2008, 51:2350-2353.
5. Ahn MY, Chung HY, Choi WS, Lee BM, Yoon S, Kim HS. Anti-tumor effect of apicidin on Ishikawa human endometrial cancer cells both in vitro and in vivo by blocking histone deacetylase 3 and 4. Int J Oncol 2010, 36:125-131.
- 1. Cheung CHY, Hsu CL, et al. "Combinatorial targeting of MTHFD2 and PAICS in purine synthesis as a novel therapeutic strategy." Cell Death Dis. 2019 Oct 17;10(11):786. PMID:31624245
- 2. Ballante F, Reddy DR, et al. "Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy." Bioorg Med Chem. 2017 Apr 1;25(7):2105-2132. PMID:28259528
- 3. Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 623.78 |
| Cas No. | 183506-66-3 |
| Formula | C34H49N5O6 |
| Solubility | Limited solubility, soluble in DMSO or ethanol |
| Chemical Name | (3S,6S,9S,12R)-3-[(2S)-butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone |
| SDF | Download SDF |
| Canonical SMILES | CCC(C)C1C(=O)N2CCCCC2C(=O)NC(C(=O)NC(C(=O)N1)CC3=CN(C4=CC=CC=C43)OC)CCCCCC(=O)CC |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
HeLa细胞 |
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制备方法 |
在DMSO中的溶解度有限。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
1 μg/mL；24小时 |
|
实验结果 |
Apicidin对HeLa细胞具有持久的抗增殖活性。于停药后48小时，Apicidin仍能保持其抗增殖活性。 |
| 动物实验 [2]: | |
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动物模型 |
Ishikawa子宫内膜癌异种移植小鼠模型 |
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给药剂量 |
5 mg/kg；腹腔注射；每日1次，持续21天 |
|
实验结果 |
于Apicidin治疗后15天，Apicidin开始显著抑制肿瘤生长。在5 mg/kg剂量下，Apicidin显著抑制肿瘤生长（高达53%）。 |
|
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Han JW, Ahn SH, Park SH, Wang SY, Bae GU, Seo DW, et al. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Res 2000,60:6068-6074. [2]. Ahn MY, Chung HY, Choi WS, Lee BM, Yoon S, Kim HS. Anti-tumor effect of apicidin on Ishikawa human endometrial cancer cells both in vitro and in vivo by blocking histone deacetylase 3 and 4. Int J Oncol 2010,36:125-131. |
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| 描述 | Apicidin是组蛋白去乙酰化酶（HDAC）的抑制剂，对HDAC3和HDAC6的IC50值分别为15.8 nM和665.1 nM。 | |||||
| 靶点 | HDAC3 | HDAC6 | ||||
| IC50 | 15.8 nM | 665.1 nM | ||||
化学结构
相关生物数据
相关生物数据
