Panobinostat，即LBH589，是一種新的和有效的基于異羥肟酸的脫乙酰酶抑制劑(DACis ),在低納摩爾濃度下抑制廣譜組蛋白脫乙酰酶(HDAC ),包括所有1、2和4類HDAC酶。根據(jù)以前的研究，它不僅通過胱天蛋白酶激活和聚(ADP-核糖)聚合酶(PARP)切割誘導(dǎo)多發(fā)性骨髓瘤(MM)細(xì)胞的凋亡，而且還以時(shí)間和劑量依賴的方式在費(fèi)城染色體陰性(Ph-)急性淋巴細(xì)胞白血病(ALL)細(xì)胞系(T細(xì)胞MOLT-4和前B細(xì)胞Reh)中誘導(dǎo)有效的細(xì)胞生長抑制、細(xì)胞周期停滯和凋亡，這與組蛋白(H3K9和H4K8)超乙?；恼T導(dǎo)、p21和p27的激活相關(guān)

產(chǎn)品性質(zhì)：

Cas No:404950-80-7

別名:帕比司他; LBH589; NVP-LBH589

化學(xué)名:(E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide

Canonical SMILES:CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)C=CC(=O)NO

分子式:C21H23N3O2

分子量:349.43

溶解度:≥ 17.47mg/mL in DMSO

儲(chǔ)存條件：Store at -20°C

注意事項(xiàng)：

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References:

[1].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)

[2].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

[3].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