Panobinostat (LBH589)
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.
Panobinostat (LBH589)是一种新型的和有效的去乙酰化酶(HDAC)抑制剂,在低浓度下抑制包括1类、2类和4类HDAC在内的一系列组蛋白去乙酰化酶(HDACs)。据报道,在费城染色体阴性(Ph-)急性淋巴细胞白血病(ALL)细胞系(T细胞MOLT-4和前B细胞Reh)中,Panobinostat通过caspase激活和PARP切割诱导细胞凋亡,以时间和剂量依赖的方式诱导细胞生长抑制、细胞周期停滞和细胞凋亡,这与诱导组蛋白(H3K9和H4K8)的超乙酰化、p21和p27的激活以及c-Myc的抑制相关。
参考文献:
Wenlin Shao, Joseph D. Growney, Yun Feng, Gregory O’Connor, Minying Pu, Wenjing Zhu, Yung-Mae Yao, Paul Kwon, Stephen Fawell and Peter Atadja. Activity of deacetylase inhibitor panobinostat (LBH589) in cutaneous T-cell lymphoma models: defining molecular mechanisms of resistance. Int. J. Cancer: 127, 2199-2208 (2010)
Laurence Catley, Ellen Weisberg, Tanyel Kiziltepe, Yu-Tzu Tai, Teru Hideshima, Paola Neri, Pierfrancesco Tassone, Peter Atadja, Dharminder Chauhan, Nikhil C. Munshi and Keneth C. Anderson. Aggresome induction by proteasome inhibitor bortezomib and α-tubulin hyperacetylation by tubulin deacetylase (TDAC) inhibitor LBH589 are synergistic in myeloma cells. Blood (2006); 108(10): 3441-3449
Anna Scuto, Mark Kirschbaum, Claudia Kowolik, Leo Kretzner, Agnes Juhasz, Peter Atadja, Vinod Pullarkat, Ravi Bhatia, Stephen Forman, Yun Yen, and Richard Jove. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood (2008); 111(10):5093-5100
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Storage | Store at -20°C |
M.Wt | 349.43 |
Cas No. | 404950-80-7 |
Formula | C21H23N3O2 |
Synonyms | Panobinostat,LBH589,LBH-589, Faridak, NVP-LBH589, |
Solubility | insoluble in H2O; insoluble in EtOH; ≥17.47 mg/mL in DMSO |
Chemical Name | (E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)C=CC(=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 |
MCF-7aro、LTEDaro、Exe-R、Let-R和Ana-R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°C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°C以下储存几个月。 |
反应条件 |
20 nM;6天 |
应用 |
用AI敏感细胞系MCF-7aro以及通过体外AI(Exe-R、Let-R和Ana-R)选择或在缺乏雌激素时长期培养获得的MCF-7aro的AI抗性变异(即LTEDaro)来研究芳香酶抑制剂(AIs)的细胞内反应以及获得AI抗性的机制。MCF-7aro、LTEDaro和三个AI抗性细胞系暴露于逐渐增加浓度的LBH589,LBH589以剂量依赖的方式抑制所有细胞系的增殖。 |
动物实验[1]: | |
动物模型 |
6-7周龄雌性去卵巢BALB/c Nu–Nu无胸腺小鼠 |
剂量 |
20 mg/kg,3次/周;腹腔注射 |
应用 |
用exemestane抗性的MCF7aro异种移植模型评估LBH589对体内AI抗性的抑制效果。LBH589显著抑制exemestane抗性肿瘤的生长,在实验结束时,LBH589处理小鼠中肿瘤的重量显著低于对照组。在LBH589处理组,没有小鼠出现明显的体重下降,表明LBH589耐受性良好。与其对肿瘤的效果一致,LBH589显著降低肿瘤细胞的增殖(Ki-67染色),并显著增加肿瘤细胞的凋亡(裂解PARP的染色)。 |
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] Kubo M, Kanaya N, Petrossian K, et al. Inhibition of the proliferation of acquired aromatase inhibitor-resistant breast cancer cells by histone deacetylase inhibitor LBH589 (panobinostat)[J]. Breast cancer research and treatment, 2013, 137(1): 93-107. |
描述 | Panobinostat (LBH589)是一种新型的广谱HDAC抑制剂,IC50值为5 nM。 | |||||
靶点 | HDAC (MOLT-4 cells) | HDAC (Reh cells) | ||||
IC50 | 5 nM | 20 nM |
质量控制和MSDS
- 批次: