cbp-2

Thalidomide-NH-CBP p300 ligand 2 (P-007) is a PROTAC-based compound engineered to degrade the proteins CBP and p300, functioning as a molecular antagonist (WO2020173440).

CBP p300 ligand 2 is a selective ligand that binds to the target protein for PROTAC[dCBP-1], a potent and selective heterobifunctional degrader of p300 CBP.

EP300 CBP ligand 2 (compound S19) serves as a specific ligand for the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). It plays a critical role in PROTAC technology by acting as a target protein ligand. By linking to an E3 ubiquitin ligase ligand via the PROTAC Linker, it facilitates the synthesis of PROTAC molecules capable of targeted protein degradation. For instance, when EP300 CBP ligand 2 is connected to the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc, it results in the formation of the PROTAC molecule dCE-2.

Thalidomide-NH-C10-Boc (compound S20) serves as a conjugate that combines the E3 ubiquitinase ligand Thalidomide with a PROTAC Linker, enabling the recruitment of Cereblon ubiquitinase. This compound facilitates the coupling of target protein ligands via the PROTAC Linker to create PROTAC molecules capable of inducing degradation. An instance of its function includes the coupling with EP300 CBP ligand 2 to form the PROTAC molecule dCE-2.

dCE-2, a PROTAC compound, specifically targets CBP EP300. It comprises several key components: the E3 ubiquitin ligase ligand Thalidomide-4-OH, the PROTAC linker tert-Butyl 11-aminoundecanoate, and the PROTAC target protein ligand EP300 CBP ligand 2. The activity of the target protein ligand is regulated by EP300 CBP ligand 1. Additionally, the conjugate of the E3 ubiquitin ligase ligand and linker is denoted as Thalidomide-NH-C10-Boc.