Vorinostat (SAHA, MK0683)
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.
Vorinostat (Suberoylanilide hydroxamic acid, SAHA)是组蛋白去乙酰化酶（HDAC）的抑制剂，在表观遗传或非表观遗传调控中起重要作用，诱导生长停滞，分化和肿瘤细胞的凋亡[1]。Vorinostat是一个小分子化合物，分子式为C14H20N2O3，分子量为264.3。HDAC抑制剂诱导细胞凋亡的主要机制是内在凋亡途径的激活。HDAC抑制剂通过调节Bcl-2家族蛋白的表达和诱导线粒体细胞色素C的释放，从而激活内在的凋亡途径，诱导细胞凋亡[2]。
参考文献：
[1] Hui-ming Z, Qian-hai D, Wei-ping C, Ru-bin L. Vorinostat, a HDAC inhibitor, showed anti-osteoarthritic activities through inhibition of iNOS and MMP expression, p38 and ERK phosphorylation and blocking NF-kB nuclear translocation. International Immunopharmacology. 2013, 17. 329-335.
[2] Norihisa U, Sayaka K, Hisanori M, Katsuhiko Y, Airo T. Requirement of p38 MAPK for a cell-death pathway triggered by vorinostat in MDA-MB-231 human breast cancer cells. Cancer Letters. 2012, 315. 112-121.
- 1. Shelby M. Knoche, Gabrielle L. Brumfield, et al. "The histone deacetylase inhibitor M344 as a multifaceted therapy for pancreatic cancer." PLoS One. 2022 Sep 20;17(9):e0273518. PMID: 36126055
- 2. Phoebe McCrorie, Jonathan Rowlinson, et al. "Detection of Label-Free Drugs within Brain Tissue Using Orbitrap Secondary Ion Mass Spectrometry as a Complement to Neuro-Oncological Drug Delivery." Pharmaceutics. 2022 Mar 5;14(3):571. PMID: 35335947
- 3. Nora-Guadalupe P Ramirez, Jeon Lee, et al. "ADAP1 promotes latent HIV-1 reactivation by selectively tuning KRAS–ERK–AP-1 T cell signaling-transcriptional axis." Nat Commun. 2022 Mar 1;13(1):1109. PMID: 35232997
- 4. Yanhong Xu, Shiqiao Peng, et al. "High doses of butyrate induce a reversible body temperature drop through transient proton leak in mitochondria of brain neurons." Life Sci. 2021 Aug 1;278:119614. PMID: 34022200
- 5. Maojun Zhou, Hao Zheng, et al. "Discovery of a novel AR/HDAC6 dual inhibitor for prostate cancer treatment." Aging (Albany NY). 2021 Feb 17;13(5):6982-6998. PMID: 33621955
- 6. Haiyang Yu, Shan Lu, et al. "TDP-43 and HSP70 phase separate into anisotropic, intranuclear liquid spherical annuli." bioRxiv. March 29, 2020.
- 7. Liu W, Song YY, et al. "Dysregulation of FOXO transcription factors in Epstein-Barr virus-associated gastric carcinoma." Virus Res. 2020;276:197808. PMID: 31712122
- 8. Emily L Morton, Christian V Forst, et al. "Transcriptional Circuit Fragility Influences HIV Proviral Fate." bioRxiv. 2018 December 23.
- 9. Feng XL, Deng HB, et al. "Suberoylanilide Hydroxamic Acid Triggers Autophagy by Influencing the mTOR Pathway in the Spinal Dorsal Horn in a Rat Neuropathic Pain Model." Neurochem Res. 2018 Dec 17. PMID: 30560396
- 10. Deng R, Zhang P, et al. "HDAC is indispensable for IFN-γ-induced B7-H1 expression in gastric cancer." Clin Epigenetics. 2018 Dec 11;10(1):153. PMID: 30537988
- 11. Kim SR, Lewis JM, et al. "BET inhibition in advanced cutaneous T cell lymphoma is synergistically potentiated by BCL2 inhibition or HDAC inhibition." Oncotarget. 2018 Jun 26;9(49):29193-29207. PMID: 30018745
- 12. Hari Prasad, Rajini Rao. "The Amyloid Clearance Defect in ApoE4 Astrocytes is Corrected by Epigenetic Restoration of NHE6." bioRxiv. 2018.January. 4 PMID: 29498802
- 13. Mirza AN, Fry MA, et al. "Combined inhibition of atypical PKC and histone deacetylase 1 is cooperative in basal cell carcinoma treatment." JCI Insight. 2017 Nov 2;2(21). pii: 97071. PMID: 29093271
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 264.3 |
| Cas No. | 149647-78-9 |
| Formula | C14H20N2O3 |
| Synonyms | SAHA, suberoylanilide hydroxamic acid, Suberanilohydroxamic acid, SAHA cpd |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥4.41 mg/mL in DMSO |
| Chemical Name | N'-hydroxy-N-phenyloctanediamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO |
| 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 |
人类皮肤T细胞淋巴瘤（CTCL）细胞系 |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
72h；IC50: 0.146 μM（HH）、2.062 μM（HuT78）、2.697 μM（MJ）、1.375 μM（MylA）、1.510 μM（SeAx） |
|
应用 |
在HH、HuT78、MJ、MylA和SeAx细胞中，vorinostat剂量依赖地减少细胞增殖，IC50值分别为0.146 μM、2.062 μM、2.697 μM、1.375 μM和1.510 μM。 |
| 动物实验[2]： | |
|
动物模型 |
Eμ-myc淋巴瘤C57BL/6小鼠 |
|
剂量 |
Eμ-myc淋巴瘤C57BL/6小鼠注射vorinostat（200 mg/kg i.p.），在指点时间点后收获淋巴细胞，并用FACS分析确定淋巴结中肿瘤细胞的百分比。 |
|
应用 |
在体内，vorinostat诱导Eμ-myc淋巴瘤的明显积累，并显示DNA片段化。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Wozniak M B, Villuendas R, Bischoff J R, et al. Vorinostat interferes with the signaling transduction pathway of T cell receptor and synergizes with PI3K inhibitors in cutaneous T-cell lymphoma. haematologica, 2010: haematol. 2009.013870. [2] Lindemann R K, Newbold A, Whitecross K F, et al. Analysis of the apoptotic and therapeutic activities of histone deacetylase inhibitors by using a mouse model of B cell lymphoma. Proceedings of the National Academy of Sciences, 2007, 104(19): 8071-8076. |
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| 描述 | Vorinostat (suberoylanilide hydroxamic acid, SAHA)是HDAC的抑制剂，IC50值约为10 nM。 | |||||
| 靶点 | HDAC | |||||
| IC50 | ~10 nM | |||||
质量控制和MSDS
- 批次:
化学结构
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