p300/cbp

PROTAC CBP P300 Degrader-1 is an effective compound that potently degrades CBP P300, significantly reducing cell viability in various cancer cell lines.

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.

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).

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.

EP300 CBP ligand 1, classified as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves a primary role in synthesis applications.

dCBP-1 is a chemical degrader of p300 CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300 CBP. Degradation of p300 CBP by dCBP-1 leads to effective multiple myeloma cell killing.

Thalidomide-NH-PEG4-COOH is a conjugate comprising an E3 ligase ligand-linker, utilized in the synthesis of dCBP-1. dCBP-1 itself functions as a powerful and selective heterobifunctional degrader targeting p300 CBP.

QC-125 is a PROTAC degrader specifically targeting p300 CBP.

Piperidine-GNE-049-N-Boc is a ligand that specifically binds to the target protein dCBP, facilitating its degradation by a selective and potent heterobifunctional degrader, p300 CBP.

MJP6412 acts as an effective degrader of p300 CBP, exhibiting DC50 values of 1.6 nM for p300 and 1.2 nM for CBP. It plays a significant role in cancer research.

QC-124 is a PROTAC degrader specifically targeting p300 CBP.

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP p300, exhibiting half-maximal degradation concentration (DC50) values of 0.05 nM for CBP and 0.2 nM for p300. The compound comprises lenalidomide (the cereblon ligand), a connecting linker, and GNE-207 (the bromodomain inhibitor). JET-209 is utilized in cancer research [1].