Chemical Structure : SETDB1 activator (R,R)-59
CAS No.:
2755823-12-0
SETDB1 activator (R,R)-59
((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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
(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.
Physicochemical Properties
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M.Wt
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469.59
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Formula
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C28H31N5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C1C(NC=C2)=C2N=C(N[C@H]3CN(C)C[C@@H](C4=CC=C(OCC5=CC=CC=C5)C=C4)C3)N1CC=C
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