Chemical Structure : SETDB1 activator (R,R)-59
CAS No.:
2755823-12-0
SETDB1 activator (R,R)-59
((R,R)-59)
货号: 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.
大包装，大折扣！
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
(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.
物理化学性质&存储条件
|
分子量
|
469.59
|
|
分子式
|
C28H31N5O2
|
|
外观性状
|
Solid
|
|
CAS No.
|
|
|
储存条件
|
- 固体粉末
-
-20°C 12 个月; 4°C 6 个月
|
- 配置液
-
-80°C 6 个月; -20°C 6 个月
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
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
|
