Favorite  |  Set Home
Product name : UNC669
Item : CR1784
Price : 200mg, $745; 500mg, $1485
contact : Send inquiry to: info@acesobio.com
Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 1314241-44-5
 Enlarge Image                   Back
             [Next Product]→


Details:
 Chemical Information
M.Wt 338.24 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C15H20BrN3O
CAS No 1314241-44-5
Solubility

DMSO



Biological Activity of UNC 669

 

UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).
IC50 value: 4.2 uM/3.1 uM (L3MBTL1/L3MBTL3) [1]
Target: L3MBTL1/L3MBTL3

 

[1]. James LI, et al. Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem. 2013 Sep 26;56(18):7358-71.
Abstract
Lysine methylation is a key epigenetic mark, the dysregulation of which is linked to many diseases. Small-molecule antagonism of methyl-lysine (Kme) binding proteins that recognize such epigenetic marks can improve our understanding of these regulatory mechanisms and potentially validate Kme binding proteins as drug-discovery targets. We previously reported the discovery of 1 (UNC1215), the first potent and selective small-molecule chemical probe of a methyl-lysine reader protein, L3MBTL3, which antagonizes the mono- and dimethyl-lysine reading function of L3MBTL3. The design, synthesis, and structure-activity relationship studies that led to the discovery of 1 are described herein. These efforts established the requirements for potent L3MBTL3 binding and enabled the design of novel antagonists, such as compound 2 (UNC1679), that maintain in vitro and cellular potency with improved selectivity against other MBT-containing proteins. The antagonists described were also found to effectively interact with unlabeled endogenous L3MBTL3 in cells.


Related Products :
EPZ004777
EPZ004777
Price: 100mg, $945; 200mg, $1485