规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥545.00 | 现货 | |
10mg | ¥545.00 | 现货 | |
50mg | ¥1818.00 | 现货 | |
200mg | ¥4272.00 | 现货 | |
500mg | ¥8909.00 | 现货 |
特色产品
- 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
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
产品性质
物理外观 | Solid |
CAS号 | 404950-80-7 |
分子式 | C21H23N3O2 |
分子量 | 349.43 |
小分子别名 | Panobinostat |
化学名称 | (E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide |
溶解度 | insoluble in H2O; insoluble in EtOH; ≥17.47 mg/mL in DMSO |
SMILES | CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)C=CC(=O)NO |
存储条件 | -20°C |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |
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 | 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) |
生物活性数据 | 5 nM | 20 nM |
生物相关数据
质量控制
操作说明
产品引用文献
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- 2. Manna PR, Ramachandran S, et al. "Expression and Function of StAR in Cancerous and Non-Cancerous Human and Mouse Breast Tissues: New Insights into Diagnosis and Treatment of Hormone-Sensitive Breast Cancer." Int J Mol Sci 2023 Jan 01;24(1) PMID: 36614200
- 3. Joseph Boyle, Derick Chiappo, et al. "Aminocoumarin-based heme oxygenase activity fluorescence probe reveals novel aspects of HO-1 regulation." Research Square. 22 Nov, 2023.
- 4. Yoichiro Kawamura, Lingyang Hua, et al. "Histone deacetylase inhibitors enhance oncolytic herpes simplex virus therapy for malignant meningioma." Biomed Pharmacother. 2022 Nov;155:113843. PMID: 36271587
- 5. Jesus Gonzalez Bosquet, Qing Zhang, et al. "Association of a novel endometrial cancer biomarker panel with prognostic risk, platinum insensitivity, and targetable therapeutic options." PLoS One. 2021 Jan 27;16(1):e0245664. PMID: 33503056
- 6. Susanna Nencetti, Doretta Cuffaro, et al. "Identification of histone deacetylase inhibitors with (arylidene) aminoxy scaffold active in uveal melanoma cell lines." J Enzyme Inhib Med Chem. 2021 Dec;36(1):34-47. PMID: 33100043
- 7. Sauradip Chaudhuri, Martha Fowler, et al. "β-Cyclodextrin-Poly (β-Amino Ester) Nanoparticles Are a Generalizable Strategy for High Loading and Sustained Release of HDAC Inhibitors." ChemRxiv. Mar 27. 2020.
- 8. 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
- 9. Martins VF, Begur M, et al. "Acute inhibition of protein deacetylases does not impact skeletal muscle insulin action." Am J Physiol Cell Physiol. 2019 Aug 28. PMID: 31461343
- 10. Simic D, Sang N. "Compounds targeting class II histone deacetylases do not cause panHDACI-associated impairment of megakaryocyte differentiation." Exp Hematol. 2019 Jan 4. pii: S0301-472X(19)30005-0. PMID: 30611870
- 11. Manna PR, Ahmed AU, et al. "Overexpression of the steroidogenic acute regulatory protein in breast cancer: Regulation by histone deacetylase inhibition." Biochem Biophys Res Commun. 2019 Feb 5;509(2):476-482. PMID: 30595381
- 12. Hacker KE, Bolland DE, et al. "The DEK Oncoprotein Functions in Ovarian Cancer Growth and Survival." Neoplasia. 2018 Dec;20(12):1209-1218. PMID: 30412857
- 13. Hari Prasad, Rajini Rao. "The Amyloid Clearance Defect in ApoE4 Astrocytes is Corrected by Epigenetic Restoration of NHE6." bioRxiv. 2018.January. 4.
- 14. Lee HM, Lee E, et al. "Drug repurposing screening identifies bortezomib and panobinostat as drugs targeting cancer associated fibroblasts (CAFs) by synergistic induction of apoptosis." Invest New Drugs. 2018 Jan 18. PMID: 29349597
- 15. Ballante F, Reddy DR, et al. "Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy." Bioorg Med Chem. 2017 Apr 1;25(7):2105-2132. PMID: 28259528
- 16. 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
- 17. Reddy DR, Ballante F, et al. "Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors." Eur J Med Chem. 2017 Feb 15;127:531-553. PMID: 28109947
- 18. Chatterjee N, Tian M, et al. "Keap1-Independent Regulation of Nrf2 Activity by Protein Acetylation and a BET Bromodomain Protein."PLoS Genet. 2016 May 27;12(5):e1006072. PMID: 27233051
- 19. Reddy DN, Ballante F, et al. "Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors." J Med Chem. 2016 Feb 25;59(4):1613-33. PMID: 26681404