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I-BET-151
7-(3,5-二甲基-4-异恶唑基)-1,3-二氢-8-甲氧基-1-[(1R)-1-(2-吡啶基)乙基]-2H-咪唑并[4,5-c]喹啉-2-酮
I-BET-151
  • 产品编号: CIR120050

  • CAS号: 1300031-49-5

  • 分子式:C23H21N5O3

  • 分子量:415.44

英文别名:
7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-Imidazo[4,5-c]quinolin-2-one
SMILES:
CC(C[C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@@H](CC1=CNC2=CC=CC=C12)C(=O)N)=O)CC(=O)O)=O)=O)CO)=O)CC1=CC=CC=C1)=O)[C@H](O)C)=O)NC([C@@H]1CCC(=O)N1)=O)C
参考文献:
Seal, J., et al.L Bioorg. Medn. Chem. Letters., 22, 2968 (2012); Mirguet, O., et al.: Bioorg. Medn. Chem. Letters, 22, 2963 (2012); Dawson, M.A., et al.: Nature., 478, 529 (2011);
I-BET 151 is part of a novel series of quinoline isoxazole BET family bromodomain inhibitors, a family of four proteins that selectively bind to aceylated lysine residues in histone. I-BET 151 play key roles in many cellular processes, including anti-inflammatory gene expression, mitosis, and viral/host interaction by controlling the conformation of histone acetylation -dependent chromatin complexes. Studies have shown that I-BET 151 increased ApoA1 expression within the nanomolar range in human hepatic cell line HepG2. The upregulation by I-BET 151 suggested potential anti-inflammatory activities upon administration.
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