Biological Activity:

TRIM24-C34 is a potent, selective and cell permeable BRPF1B and TRIM24 dual inhibitor. It binds to bromodomain BRPF1B with a Kd of 137 nM, and the transcriptional regulator TRIM24 (also an E3 ubiquitin ligase) with a Kd of 222 nM. It has very good selectivity against other 45 bromodomains. Cellular activity of TRIM24-C34 was demonstrated using FRAP assays as well as cell viability data. It showed no significant cytotoxicity in the cell lines tested.

How to Use:

In vitro: TRIM24-C34 was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Bennett J, et al. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. (2015) J Med Chem. In press.