84468-17-7Relevant articles and documents
Small-molecule inhibitor of protein kinase A as well as preparation method and application thereof
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Paragraph 0055; 0061-0062, (2020/07/02)
The invention discloses a small-molecule inhibitor of histone kinase A. The small-molecule inhibitor comprises an H89 isoquinoline precursor structure, the specific molecular formula is CxHyAzNmOnS, and in the molecular formula, x is 20 or 21, y is 20 or 22, A is F, z is 0 or 1, m is 3 or 4, and n is 2 or 4. The invention further provides small-molecule inhibitors HF89, HFC and HN89, and a PET tracer [ C] HF. The invention also provides a preparation method and an application of the related small-molecule inhibitor. A new feasible scheme is provided for early diagnosis, treatment, curative effect evaluation and the like of tumors.
Compounds for treating central nervous system degenerative diseases or brain tumor and application thereof
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Paragraph 0022, (2017/07/07)
The invention relates to compounds and a medicine composition for treating central nervous system degenerative diseases or brain tumor and application thereof. The compounds have the structure of the formula (see the formula in the description) and can se
Photo-crosslinking of clinically relevant kinases using H89-derived photo-affinity probes
Stolze, Sara C.,Liu, Nora,Wijdeven, Ruud H.,Tuin, Adriaan W.,Van Den Nieuwendijk, Adrianus M. C. H.,Florea, Bogdan I.,Van Der Stelt, Mario,Van Der Marel, Gijsbert A.,Neefjes, Jacques J.,Overkleeft, Herman S.
, p. 1809 - 1817 (2016/06/09)
The profiling of kinases using established proteomics techniques is hampered by their non-covalent mode-of-action. One way to overcome this caveat is the use of probes featuring photo-labelling groups that can be activated by UV irradiation to generate a reactive species that will establish a covalent bond to the enzyme. In this study we have used the well-known kinase inhibitor H89 as a lead for the development of probes for the affinity-based profiling of clinically relevant kinases. A labelling protocol was established for recombinant kinases and more complex protein mixtures using gel-based techniques. We also show that the probes act in a competitive manner with other kinase inhibitors.