Catalog No.: PC-20832Not For Human Use, Lab Use Only.
(R,R)-59 is a small-molecule ligand activator for methyltransferase SETDB1 Triple Tudor Domain (3TD reader domain) with binding IC50 of 1.2 uM in TR-FRET assays, specifically promotes in vitro SETDB1-mediated methylation of lysine 64 of protein kinase Akt1.
(R,R)-59 is a small-molecule ligand activator for methyltransferase SETDB1 Triple Tudor Domain (3TD reader domain) with binding IC50 of 1.2 uM in TR-FRET assays, specifically promotes in vitro SETDB1-mediated methylation of lysine 64 of protein kinase Akt1.
(R,R)-59 shows a Kd of 4.8 uM in a direct binding assay using surface plasmon resonance (SPR) assays, (S,S)-59, the enantiomer of (R,R)-59, is not able to displace the H3K9Me2K14Ac (aa 1-20) peptide.
(R,R)-59 (10 uM) increases Akt1 methylation and subsequent phosphorylation in HEK293T cells transfected with HA-Akt1.
(R,R)-59 (2.5 and 5 uM) promoted cell proliferation in MDA-MB-231 cells, bot not under high concentrations (>5 uM).
(R,R)-59 is the first SETDB1 small-molecule positive activator for the methyltransferase activity of Akt-1.
