L3MBTL antagonist,potent and selective
CAS：1314241-44-5
分子式：C15H20BrN3O
分子量：338.24
纯度：98%
存储：Store at -20°C

Background:

UNC 669 is a potent antagonist of L3MBTL1 (IC50=4.2 μM) and L3MBTL3 (IC50=3.1 μM).

There is less bio-data supported for UNC669. UNC1679 is an analog of UNC669. UNC1215 is the first potent and selective antagonism of a methyl-lysine reader protein, L3MBTL3, which antagonizes the mono- and dimethyl-lysine reading function of L3MBTL3. [1]

Lysine methylation is a key epigenetic landmark, the dysregulation of which is related to many diseases. UNC1679 maintains 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. [1]

Reference:
1.  James LI, Korboukh VK, Krichevsky L 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. doi: 10.1021/jm400919p. Epub 2013 Sep 16.