A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
- A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
- Ibrahim M. El-Deeb; 정수진; 박병선; 유영준; 최기항; 양영목; 이상우; 김인태; 한동근; 이소하
- Staurosporine derivative; Selectivity filter; Kinase selectivity; Cancer
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 32, NO 5, 1709-1714
- KIST301135 was semi-synthetically prepared by the reaction of Staurosporine with triphosgene in anhydrous
dichloromethane. The structure of KIST301135 was confirmed by 1H NMR, 13C NMR, and high resolution
mass spectrum. KIST301135 was initially tested in a single dose duplicate mode at a concentration of 20 nM
over a panel of 53 kinases against Staurosporine as a positive control. KIST301135 has showed inhibitions
above 75% in only 2 kinases (FLT3 and JAK3 kinases) of the 53 tested kinases, while Staurosporine has
showed inhibitions above 80% in about 62% of the tested kinases. KIST301135 was retested at a 5-dose testing
mode over the 9 kinases inhibited by percentages over 20 at the single dose testing in order to determine its IC50
values. KIST301135 has shown much improved kinase inhibitory selectivity relative to Staurosporine in its
potency at JAK3 kinase and CAMK2b kinase.
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