17 research outputs found
Research Reference Document 06/01 : Anadromous Alosid Restoration in the Androscoggin River Watershed Semi-Annual Report (January 1, 2006 - June 30, 2006)
https://digitalmaine.com/dmr_research_reference_documents/1007/thumbnail.jp
Research Reference Document 06/01 : Anadromous Alosid Restoration in the Androscoggin River Watershed Semi-Annual Report (January 1, 2006 - June 30, 2006)
https://digitalmaine.com/dmr_research_reference_documents/1007/thumbnail.jp
Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties
The development of a series of potent and highly selective casein kinase 1δ/ε (CK1δ/ε) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highly kinase selective inhibitors, including SR-2890 and SR-3029, which have IC(50) ≤ 50 nM versus CK1δ. The two lead compounds have ≤ 100 nM EC(50) values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines