计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
在色谱分析、有机合成和交叉偶联反应领域已被 18 篇同行评审文献引用。
Suberoylanilide Hydroxamic Acid (SAHA) is a potent histone deacetylase (HDAC) inhibitor that has been shown to inhibit proliferation and cause cell cycle arrest at G1. Experiments suggest that SAHA also causes morphological changes, such as enlargement and flattening of the cytoplasm, resulting in growth inhibition. Treatment of cells with SAHA also decreases the expression of anti-apoptosis proteins Bcl-xL and survivin.
A potent HDAC inhibitor; also causes cell cycle arrest at G1
SAHA可用于研究基因调控、转录调控和细胞信号转导。
Information
In vitro
Vorinostat inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively. Vorinostat also results in a marked hyperacetylation of histone H4. Vorinostat inhibits the growth of three prostate cancer cell lines LNCaP, PC-3 and TSU-Pr1 at micromolar concentrations (2.5-7.5 μM), and induces dose-dependent cell death in LNCaP cells. Vorinostat treatment in MCF-7 cells inhibits cell proliferation at an IC50 of 0.75 μM resulting in the accumulation of cells in the G1 and G2-M phase of the cell cycle. Vorinostat also induces differentiation in the estrogen receptor-negative cell line SKBr-3 and the retinoblastoma-negative cell line MDA-468. Vorinostat treatment at 1 μM for 8 hours or more is sufficient to irreversibly induce apoptosis of human multiple myeloma (MM) cells. The gene expression profiles of Vorinostat treated MM cells are not hallmarked by global transcriptional activation, but by coordinated transcriptional changes of specific functional groups of genes such as cytokine-induced proliferative/survival signaling cascades, oncogenes-tumor suppressor genes, regulators of apoptosis, DNA synthesis-repair and cell cycle, and proteasome-ubiquitin function.
In vivo
Administration of Vorinostat (~100 mg/kg/day) significantly inhibits the growth of CWR22 human prostate xenografts in nude mice with tumor reductions of 78%, 97% and 97%, at doses of 25 mg/kg/day, 50 mg/kg/day and 100 mg/kg/day, respectively, compared with control. Vorinostat induces the accumulation of acetylated core histones and prostate-specific antigen mRNA expression in CWR22 cells, resulting in higher levels of serum prostate-specific antigen than predicted from tumor volume alone. Oral administration of Vorinostat (0.67g/L) crosses the blood-brain barrier, increases histone acetylation in the brain, and dramatically improves the motor impairment in the R6/2 mice model of Huntington\'s disease.
Cell Data
cell lines:
Concentrations:Dissolved in DMSO, final concentrations ~7.5 μM
Incubation Time:1, 2, 3 and 4 days
Powder Purity:≥99%
| ALogP | 1.9 |
|---|
H341: 怀疑引起遗传缺陷
H302: 吞食有害
H400: 对水生生物有剧毒
H410: 对水生生物有剧毒并具有长期持续影响
H372: 通过长时间或反复暴露对器官造成损害
H360: 可能损害生育力或未出生的孩子
P273: 避免释放到环境中。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
P281: 根据需要使用个人防护设备。
P270: 使用本产品时,请勿进食、饮水或吸烟。
P391: 收集溢出物
P330: 漱口
P203: 使用前,获取、阅读并遵守所有安全说明。
P301+P317: 如果被吞咽:请寻求医疗帮助。
P318: 如果暴露或担心,请就医。
P319: 如果你感到不适,请寻求医疗帮助。
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | V407894 |
| 1. Lei Hou, Yunchang Zhang, Ying Huang, Zhen Fang, Guangze Sang, Tianheng Chen, Zhiqiang Ma, Feng Yang. (2022) Coupling Chlorin-Based Photosensitizers and Histone Deacetylase Inhibitors for Photodynamic Chemotherapy. MOLECULAR PHARMACEUTICS, [PMID:35758904] [10.1021/acs.molpharmaceut.2c00170] |
| 2. Jia Man, Xiaojie Wang, Jianyong Li, Xiaoyang Cui, Zesheng Hua, Jianfeng Li, Zebing Mao, Shanguo Zhang. (2022) Intravenous Calcium Alginate Microspheres as Drug Delivery Vehicles in Acute Kidney Injury Treatment. Micromachines, 13 (4): (538). [PMID:35457843] [10.3390/mi13040538] |
| 3. Yingjie Yu, Bingkai Wang, Miao Sun, Yunchang Zhang, Lei Hou, Sizhen Wang, Tianheng Chen, Feng Yang, Zhiqiang Ma. (2022) Lysosomal activable Vorinostat carrier-prodrug self-assembling with BPQDs enables photothermal oncotherapy to reverse tumor thermotolerance and metastasis. INTERNATIONAL JOURNAL OF PHARMACEUTICS, [PMID:35202725] [10.1016/j.ijpharm.2022.121580] |
| 4. Miao Jiefei, Meng Chi, Wu Hongmei, Shan Wenpei, Wang Haoran, Ling Changchun, Zhang Jinlin, Yang Tao. (2021) Novel Hybrid CHC from β-carboline and N-Hydroxyacrylamide Overcomes Drug-Resistant Hepatocellular Carcinoma by Promoting Apoptosis, DNA Damage, and Cell Cycle Arrest. Frontiers in Pharmacology, [PMID:33536926] [10.3389/fphar.2020.626065] |
| 5. Shanguo Zhang, Xiaojie Wang, Jia Man, Jianyong Li, Xiaoyang Cui, Chuanwei Zhang, Weichen Shi, Donghai Li, Song Zhang, Jianfeng Li. (2020) Histone Deacetylase Inhibitor-loaded Calcium Alginate Microspheres for Acute Kidney Injury Treatment. ACS Applied Bio Materials, [PMID:35021777] [10.1021/acsabm.0c00874] |
| 6. Qian Zhu, Lixin Jia, Zhongfei Gao, Chunming Wang, Haoyang Jiang, Junfeng Zhang, Lei Dong. (2014) A Tumor Environment Responsive Doxorubicin-Loaded Nanoparticle for Targeted Cancer Therapy. MOLECULAR PHARMACEUTICS, [PMID:24735448] [10.1021/mp4007776] |
| 7. Weiwei Jiang, Yuwei Cheng, Lei Hou, Ying Huang, Sizhen Wang, Yunchang Zhang, Tao Jiang, Feng Yang, Zhiqiang Ma. (2024) A dual-prodrug nanogel combining Vorinostat and Pyropheophorbide a for a high efficient photochemotherapy. INTERNATIONAL JOURNAL OF PHARMACEUTICS, [PMID:38977163] [10.1016/j.ijpharm.2024.124422] |
| 8. Penghui Du, Wen Liu, Qiang Zhang, Peng Zhang, Chen He, Quan Shi, Ching-Hua Huang, Junjian Wang. (2023) Transformation of dissolved organic matter during UV/peracetic acid treatment. WATER RESEARCH, [PMID:36738558] [10.1016/j.watres.2023.119676] |
| 9. Yaowei Guo, Jin Liu, Qinglin Tang, Cuicui Li, Yanying Zhang, Yao Wang, Yanxin Wang, Yupeng Bi, Christopher D. Snow, Matt J. Kipper, Laurence A. Belfiore, Jianguo Tang. (2022) Lanthanide (Eu3+/Tb3+)-Loaded γ-Cyclodextrin Nano-Aggregates for Smart Sensing of the Anticancer Drug Irinotecan. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23 (12): (6597). [PMID:35743042] [10.3390/ijms23126597] |
| 10. Yue Wei, Si Wu, Zhenqi Liu, Jingsheng Niu, Ya Zhou, Jinsong Ren, Xiaogang Qu. (2022) Tumor associated macrophages reprogrammed by targeted bifunctional bioorthogonal nanozymes for enhanced tumor immunotherapy. Materials Today, [10.1016/j.mattod.2022.01.024] |
| 11. Rui Li, Li Xie, Lei Li, Xiaojiao Chen, Tong Yao, Yuanxin Tian, Qingping Li, Kai Wang, Chenyang Huang, Cui Li, Yifan Li, Hongwei Zhou, Neil Kaplowitz, Yong Jiang, Peng Chen. (2021) The gut microbial metabolite, 3,4-dihydroxyphenylpropionic acid, alleviates hepatic ischemia/reperfusion injury via mitigation of macrophage pro-inflammatory activity in mice. Acta Pharmaceutica Sinica B, [PMID:35127379] [10.1016/j.apsb.2021.05.029] |
| 12. Pisano S., Wang X., Garcia-Parra J., Gazze A., Edwards K., Feltracco V., Hu Y., He L., Gonzalez D., Francis L. W., Conlan R. S., Li C.. (2020) Nanomicelles potentiate histone deacetylase inhibitor efficacy in vitro. Cancer Nanotechnology, 11 (1): (1-17). [10.1186/s12645-020-00070-8] |
| 13. Xie Qiu-shi, Zhang Jia-xin, Liu Ming, Liu Pei-hua, Wang Zhong-jian, Zhu Liang, Jiang Ling, Jin Meng-meng, Liu Xiao-nan, Liu Li, Liu Xiao-dong. (2020) Short-chain fatty acids exert opposite effects on the expression and function of p-glycoprotein and breast cancer resistance protein in rat intestine. ACTA PHARMACOLOGICA SINICA, 42 (3): (470-481). [PMID:32555444] [10.1038/s41401-020-0402-x] |
| 14. Zhihong Yao, Shishi Li, Zifei Qin, Xiaodan Hong, Yi Dai, Baojian Wu, Wencai Ye, Frank J. Gonzalez, Xinsheng Yao. (2017) Characterization of human UDP-glucuronosyltransferases responsible for glucuronidation and inhibition of norbakuchinic acid, a primary metabolite of hepatotoxicity and nephrotoxicity component bakuchiol in Psoralea corylifolia L.. RSC Advances, 7 (83): (52661-52671). [10.1039/C7RA10376J] |
| 15. Dong Shanshan, Li Mu, Chen Yinguang. (2017) Inherent humic substance promotes microbial denitrification of landfill leachate via shifting bacterial community, improving enzyme activity and up-regulating gene. Scientific Reports, 7 (1): (1-10). [PMID:28939832] [10.1038/s41598-017-12565-3] |
| 16. Xiao-Li Zheng, Zhi-Di Li, Kai-Zhi Luo, Yang-Ling Li, Ye-Han Liu, Shu-Ying Shen, Fei-Yan Shen, Wan-Yan Li, Guo-Qing Chen, Chong Zhang, Ling-Hui Zeng. (2024) POLR2J expression promotes glioblastoma malignancy by regulating oxidative stress and the STAT3 signaling pathway. American Journal of Cancer Research, [PMID:38859843] [10.62347/JEWM7691] |
| 17. Lu Hui, Fu Wenying, Xia Yiqun, Yan Ying, Shu Chongchong, Chen Yinghua, Xu Chenxin, Zheng Peisen, Shen Xin, Cui Ri, Zou Peng, Ni Daoyong. (2025) Panobinostat potentiates adagrasib-induced cell death by triggering autophagy in human non-small cell lung cancer. Cell Death Discovery, 11 (1): (1-16). [PMID:40750601] [10.1038/s41420-025-02657-9] |
| 18. Yanhong Guo, Shuhao Xu, Xue Guo, Jing Xu, Zhenyu Li, Ying Wang, Zhenhao Li, Zheyong Xue. (2026) Synergistic effects of exogenous inducers on ganoderic acid accumulation in Ganoderma lucidum: optimization and transcriptomic analysis. Medicinal Plant Biology, 5 (1): [10.48130/mpb-0025-0039] |