AR-42 (OSU-HDAC42)
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ¥860.00 | 现货 | |
| 2mg | ¥326.00 | 现货 | |
| 5mg | ¥733.00 | 现货 | |
| 10mg | ¥1520.00 | 现货 | |
| 50mg | ¥4227.00 | 现货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
AR-42 (OSU-HDAC42,CAS号935881-37-1),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
产品性质
| 物理外观 | Solid |
| CAS号 | 935881-37-1 |
| 分子式 | C18H20N2O3 |
| 分子量 | 312.36 |
| 小分子别名 | AR-42 |
| 化学名称 | N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide |
| 溶解度 | insoluble in EtOH; insoluble in H2O; ≥15.62 mg/mL in DMSO |
| SMILES | CC(C)[C@H](C(Nc(cc1)ccc1C(NO)=O)=O)c1ccccc1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | AR-42是HDAC的抑制剂,IC50值为30 nM。 |
| 靶点 | HDAC |
| 生物活性数据 | 30 nM |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 2 篇科研文献
- 1.Bagnall NH, Hines BM, et al."Insecticidal activities of histone deacetylase inhibitors against a dipteranparasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017Apr;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



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