Dana-farber-cancer Institute Inc.

Altius Institute for Biomedical Sciences

Alexander Federation

Jun Qi

James Elliott Bradner

James Bradner

John A Stamatoyannopoulos

Anthony Varca

Zoe Jacobson

James E Bradner

Disclosed herein are methods for solubilizing and isolating nuclear proteins from cells.

Isolation and characterization of the nuclear proteome

Provided herein are compounds useful as inhibitors of CBX. Also described are pharmaceutical compositions and medical uses of these compounds.

Chromobox protein inhibitors and uses thereof

The present invention relates to compound that bind Histone H3-lysine79 (H3K79) methyl transferase (DOTIL). The disclosed compounds are useful as for assessing the activity of DOTIL and for identifying inhibitors of DOTIL. Described herein are probes useful for both assessing the activity of DOTIL and identifying inhibitors of DOTIL. These probes can be used in various assays, including Amplified Luminescent Proximity Homogeneous Assays ('ALPHA' assays), Differential Scanning Fluorimetry (DFS) Assay, and Fluorescence Polarization (FP) assays used for high-throughput screening (HTS) for small molecule drug discovery. The compounds can also be used as a pull down agent for target identification.

DOT1L probes

Provided herein are inhibitors of DOT1L of formula (I) useful for treating diseases or disorders associated with DOT1L: in which Ris defined in the specification. An exemplary DOT1L inhibitor provided herein exhibits a biological half-life of 12.6 h. Methods for treating diseases associated with DOT1L are also provided.

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Boston, MA, United States of America

Alexander Federation