DS17701585 is a Highly Selective, Orally Active EP300 and CBP Inhibitor
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.15, 0.040, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. Besides, DS17701585 has the potential for the research of cancer. EP300 and its paralog CBP play an important role in post-translational modification as...
L-Moses Disrupts PCAF-Brd Histone H3.3 Interaction
Bromodomains proteins (Brds) bind to acetylated lysines (KAc) through the Brd acetyllysine-binding site. Misregulation of these proteins is linked to the onset and progression of multiple disease states. They include cancer, HIV infection, and neuroinflammation. The p300/CBP-associated factor, PCAF (KAT2B), is a multi-domain protein. It contains a single Brd,...