Uses
UNC 1215 is ; a potent, selective antagonist of L3MBTL3 with cellular activity. UNC1215 binds the MBT domains of L3MBTL3 with a Kd of 120 nM, competitively displacing mono- or dimethyl-lysine containing peptides
Biological Activity
UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity. Lethal (3) malignant brain tumor-like protein 3 (L3MBTL3) is a putative polycomb group (PcG) protein with gene-repressing activity, a member of the MBT family of methyllysine binders. Methyl-lysine binding proteins are a family of proteins th at are important epigenetic regulators th at “read” the post-translational methylation state of histone lysine residues and modulate protein-protein interactions th at regulate gene expression. UNC1215 has an IC50 of 20 nM and > 100-fold selectivity over 13 HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC1215 showed a significant decrease in FRAP recovery (Fluorescence Recovery After Photobleaching) time below 1 microM in cells using GFP-L3MBTL3. For full characterization details, please visit the
UNC1215 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit
sigma.com/sgc
