606-25-7Relevant articles and documents
A novel small molecular STAT3 inhibitor, LY5, inhibits cell viability, cell migration, and angiogenesis in medulloblastoma cells
Xiao, Hui,Bid, Hemant Kumar,Jou, David,Wu, Xiaojuan,Yu, Wenying,Li, Chenglong,Houghton, Peter J.,Lin, Jiayuh
, p. 3418 - 3429 (2015)
Signal transducers and activators of transcription 3 (STAT3) signaling is persistently activated and could contribute to tumorigenesis of medulloblastoma. Numerous studies have demonstrated that inhibition of the persistent STAT3 signaling pathway results in decreased proliferation and increased apoptosis in human cancer cells, indicating that STAT3 is a viable molecular target for cancer therapy. In this study, we investigated a novel non-peptide, cell-permeable small molecule, named LY5, to target STAT3 in medulloblastoma cells.LY5inhibited persistentSTAT3phosphorylation and induced apoptosis in human medulloblastoma cell lines expressing constitutive STAT3 phosphorylation. The inhibition of STAT3 signaling by LY5 was confirmed by down-regulating the expression of the downstream targets of STAT3, including cyclin D1, bcl-XL, survivin, and micro-RNA-21. LY5 also inhibited the induction of STAT3 phosphorylation by interleukin-6 (IL-6), insulin-like growth factor (IGF)-1, IGF-2, and leukemia inhibitory factor in medulloblastoma cells, but did not inhibitSTAT1 and STAT5 phosphorylation stimulated by interferon-γ (IFN-γ) and EGF, respectively. In addition, LY5 blocked the STAT3 nuclear localization induced by IL-6, but did not block STAT1 and STAT5 nuclear translocation mediated by IFN-γ and EGF, respectively. A combination of LY5 with cisplatin or x-ray radiation also showed more potent effects than single treatment alone in the inhibition of cell viability in human medulloblastoma cells. Furthermore, LY5 demonstrated a potent inhibitory activity on cell migration and angiogenesis. Taken together, these findings indicate LY5 inhibits persistent and inducible STAT3 phosphorylation and suggest that LY5 is a promising therapeutic drug candidate for medulloblastoma by inhibiting persistent STAT3 signaling.
Li et al.
, p. 3118,3119, 3120 (1975)
Compound and medical application thereof in novel coronavirus pneumonia
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Paragraph 0059-0062, (2021/06/09)
The invention relates to the field of medicinal chemistry and pharmacotherapeutics, in particular to a compound and medical application of the compound in novel coronavirus pneumonia, and belongs to the technical field of pharmacy. The compound is a compound shown in a formula I or a formula II, or pharmaceutically acceptable salt or ester of the compound. The invention relates to application in preparation of medicines for preventing and/or treating diseases related to novel coronavirus pneumonia.
Compound and medical application thereof in colorectal cancer
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Paragraph 0074-0077; 0094; 0100-0101; 0110-0111; 0117-0118, (2021/06/13)
The invention relates to the field of medicinal chemistry and pharmacotherapeutics, in particular to a compound and medical application thereof in colorectal cancer, belongs to the technical field of pharmacy, and relates to application in tumor-related activity and the like, in particular to a compound shown in a formula I or a formula II or pharmaceutically acceptable salt or ester thereof, in particular to application in preparation of medicines for preventing and/or treating tumor-related diseases, especially colorectal cancer.