CAS: 1310693-92-5; N-Hydroxy-4-((2-Methyl-1,2,3,4-Tetrahydro-5H-Pyrido[4,3-B]Indol-5-yl)Methyl)Benzamide Hydrochloride

该化合物是一种选择性的,强大的抑制乙酰酶6(HDAC6)的强效抑制剂,其IC50值为~15 nM. 它表明HDAC6相对于其他HDAC异形具有高度的特性,使其成为研究HDAC6代管细胞过程的宝贵工具.该化合物在研究中被广泛使用,以调查HDAC6在蛋白聚合,...

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    1: Wang M, Gao M, Miller KD, Sledge GW, Zheng QH. [11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1569-74. doi: 10.1016/j.bmcl.2011.12.136. Epub 2012 Jan 10. doi: 10.1158/1535-7163.MCT-14-0548. Epub 2014 Dec 12. doi: 10.1186/s12935-014-0090-z. eCollection 2014.
    4: Leung E, Kim JE, Rewcastle GW, Finlay GJ, Baguley BC. Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. Cancer Biol Ther. 2011 Jun 1;11(11):938-46. Epub 2011 Jun 1.
    5: Dolman ME, Westerhout EM, Hamdi M, Schellens JH, Beijnen JH, Sparidans RW. Liquid chromatography-tandem mass spectrometric assay for the PI3K/mTOR inhibitor GSK2126458 in mouse plasma and tumor homogenate. J Pharm Biomed Anal. 2015 Mar 25;107:403-8. doi: 10.1016/j.jpba.2015.01.026. Epub 2015 Jan 19. doi: 10.1124/jpet.115.229393. Epub 2015 Nov 24.

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    参考文献:10.1186/s13148-021-01037-1
    摘要:Dominici C, Sgarioto N, Yu Z, Sesma-Sanz L, Masson J, Richard S, Raynal NJ-. Synergistic effects of type I PRMT and PARP inhibitors against non-small cell lung cancer cells. Clinical Epigenetics. 2021 Mar 10;13(1):54. doi: 10.1186/s13148-021-01037-1.
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