UNC 669

The Uses of UNC 669

(5-Bromopyridin-3-yl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone is a selective inhibitor of malignant brain tumor (MBT).

Definition

ChEBI: (5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone is an aromatic carboxylic acid and a pyridinemonocarboxylic acid.

Biological Activity

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]

References

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.