UNC1215 : 2:2 dimer formation of L3MBTL3

Structure

Information

Protein target names: L3MBTL3

Mechanism of action: 2:2 dimer formation

Recommended in-cell concentration:
100 nM - 1 uM

In Vitro Validations

Uniprot ID: Q96JM7
Target Class: Epigenetics
Target SubClass: Malignant brain tumor Reader
Potency: Kd
Potency Value: 120 nM
Potency Assay: ITC
PDB ID for probe-target interaction (3D structure): 4FL6

DOI Reference: 10.1038/nchembio.1157

Uniprot ID: Q96JM7
Target Class: Epigenetics
Target SubClass: Malignant brain tumor Reader
Potency: IC50
Potency Value: 40 nM
Potency Assay: Alpha screen methylated histone peptide competition assay
PDB ID for probe-target interaction (3D structure): --

DOI Reference: 10.1038/nchembio.1157

In Cell Validations

In Vivo Data

No in Vivo Validations

Reagent authentication certificate: PDF image

SERP Reviews


22 Jun 2016
In Cell Rating

This probe seems to have a very nice selectivity towards L3MBTL3. UNC1215 is nontoxic at concentration well above the EC50.

14 Jun 2016
In Cell Rating
23 Jun 2016
In Cell Rating
In Model Organisms

As of June 2016, this is the first and only potent and selective inhibitor of L3MBTL3 with activity in cells. This looks like a good compound to probe this target's disease relevance and biology. The authors have characterized its off target activities as comprehensively as can be expected, including kinases, secondary pharmacology, epigenetic enzyme panels and cellular target pull-down experiments, and the data supports UNC1215 as a potent and selective inhibitor.