KG-501

Description: KG-501 is a potent inhibitor of CREB (cAMP response element-binding protein) with an IC50 of 6.89 uM. KG-501 (2-naphthol-AS-E-phosphate), targeted a surface distal to the CREB binding groove that includes Arg-600, a residue that is required for the CREB:CBP interaction. When added to live cells, KG-501 disrupted the CREB: CBP complex and attenuated target gene induction in response to cAMP agonist. These results demonstrate the ability of small molecules to interfere with second-messenger signaling cascades by inhibiting specific protein-protein interactions in the nucleus.

References: Proc Natl Acad Sci U S A. 2004 Dec 21; 101(51):17622-7; PLoS One. 2015 Apr 21; 10(4):e0122628.