AR-42 (OSU-HDAC42)
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.
AR-42 (OSU-HDAC42),hydroxamate-tethered phenylbutyrate的衍生物,是一种新型有效的组蛋白去乙酰化酶(HDAC)抑制剂,有效抑制HDAC的活性,IC50值为16 nM,诱导组蛋白H3乙酰化,α-微管蛋白乙酰化和p21的上调,这些被视为HDAC抑制的标志性指标。据报道,AR-42调节几个细胞凋亡抑制剂以及细胞存活调节剂,包括Akt、Bcl-xL、Bax、Ku70和Surviving,通过对PI3K/Akt信号通路的至少部分抑制,对多种肿瘤类型具有有效的抗肿瘤活性,如人前列腺癌和肝癌。
参考文献:
Matthew L. Bush†, Janet Oblinger†, Victoria Brendel, Griffin Santarelli, Jie Huang, Elena M. Akhmametyeva, Sarah S. Burns, Justin Wheeler, Jeremy Davis, Charles W. Yates, Abhik R. Chaudhury, Samuel Kulp, Ching-Shih Chen, Long-Sheng Chang, D. Bradley Welling, and Abraham Jacob. AR42, a novel histone deacetylase inhibitor, as a potential therapy for vestibular schwannomas and meningiomas. Neuro-Oncology 13(9):983–999, 2011
Aaron M. Sargeant, Robert C. Rengel, Samuel K. Kulp, et al. OSU-HDAC42, a Histone Deacetylase Inhibitor, Blocks Prostate Tumor Progression in the Transgenic Adenocarcinoma of the Mouse Prostate Model Cancer Res 2008;68:3999-4009.
Qiang Lu, Da-Sheng Wang, Chang-Shi Chen, Yuan-Dong Hu, and Ching-Shih Chen. Structure-Based Optimization of Phenylbutyrate-Derived Histone DeacetylaseInhibitors. J. Med. Chem. 2005, 48, 5530-5535
- 1.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
- 2.Park, Jeenah, et al. "Epigenetic modulation with histone deacetylase inhibitors in combination with immunotherapy." Epigenomics 7.4 (2015): 641-652. PMID:26111034
Storage | Store at -20°C |
M.Wt | 312.36 |
Cas No. | 935881-37-1 |
Formula | C18H20N2O3 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥15.62 mg/mL in DMSO |
Chemical Name | N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide |
SDF | Download SDF |
Canonical SMILES | CC(C)C(C1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)C(=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。 |
激酶实验 [1]: | |
体外HDAC试验 |
使用HDAC测定试剂盒分析HDAC活性。DU-145核提取物具有丰富的HDAC活性,可以使结合于链霉素琼脂糖珠的生物素化[3H]-乙酰组蛋白H4多肽脱去乙酰基。通过测量释放到上清液中的[3H]-乙酸盐计算HDAC活性。以丁酸钠 (0.25 ~ 1 mM) 为阳性对照。 |
细胞实验 [1]: | |
细胞系 |
DU-145细胞 |
制备方法 |
在DMSO中的溶解度大于10 mM。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 |
10 ~ 1000 nM;96小时 |
实验结果 |
AR-42抑制DU-145细胞生长,其IC50值为0.11 μM。 |
动物实验 [2]: | |
动物模型 |
皮下接种PC-3细胞的雄性NCr无胸腺裸鼠 |
给药剂量 |
25 mg/kg,每日1次,或50 mg/kg,每日1次,隔天给药;口服给药,持续28天 |
实验结果 |
在剂量为25 mg和50 mg下,AR-42抑制PC-3肿瘤异种移植物生长(分别为52%和67%)。 |
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]. Lu Q, Wang DS, Chen CS, Hu YD, Chen CS. Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5. [2]. Kulp SK, Chen CS, Wang DS, Chen CY, Chen CS. Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer. Clin Cancer Res. 2006 Sep 1;12(17):5199-206. |
描述 | AR-42是HDAC的抑制剂,IC50值为30 nM。 | |||||
靶点 | HDAC | |||||
IC50 | 30 nM |
质量控制和MSDS
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