Profiling of geldanamycin activity against KDMs using ALPHA screen
(A) 17-position of benzoquinone moieties of Geldanamycin, 17-DMAG, 17-AAG and 17-AG are circled (structures were obtained from htps://scifinder.cas.org).
(B) Phylogenetic tree of KDMs (left) and KDM selectivity profiling of geldanamycin, 17-DMAG, 17-AAG AND 17-AG at 5μM (right) assayed by ALPHA Screen.
(C) IC50 of geldanamycin (GA), 17-DMAG and 17-AAG for selected KDMs assayed by ALPHA Screen.
(D-E) Dose-response curve of geldanamycin, 17-DMAG and 17-AAG against KDM4B and KDM6B.
See also Figure S3.