Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : SETDB1 activator (R,R)-59
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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
(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.
| M.Wt | 469.59 | |
| Formula | C28H31N5O2 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
