CBP

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.

CBP/p300ligand 4 (Compound 4) is an orally active inhibitor of the CBP/p300 bromodomain, with an IC50 of 91.4 nM. It serves as the target protein ligand for PROTACXYD190.

CBP/p300 ligand 5 is a target protein ligand of XYD129, useful for researching acute myeloid leukemia (AML).

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).

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 the target protein ligand for PROTAC dCBP-1, a potent and selective p300/CBP degrader.

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

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.

CBPD-409 is an orally active CBP/p300 degrader with a DC50 of 0.2–0.4 nM. It exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP, and 22Rv1, with an IC50 of 1.2–2.0 nM. Additionally, CBPD-409 shows antitumor activity.

CBPD-268 is an effective orally active CBP/p300 PROTAC degrader, with a DC50 value of ≤ 0.03 nM. It induces degradation of CBP/p300 and inhibits cell growth, exhibiting antitumor activity. Additionally, CBPD-268 shows potential for research in AR-positive prostate cancer.

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.

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

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

MNN-02-155 is a bivalent molecular glue that can simultaneously interact with both p300/CBP and BCL6. It effectively induces the activation of BCL6-targeted reporter genes and promotes cell death. This compound is used in the research of diffuse large B-cell lymphoma (DLBCL).

BRD4 ligand 6 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). It serves as a key component in synthesizing the PROTAC CBP/BRD4 degrader-1.

TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.

Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader. It consists of the CRBN ligand Pomalidomide, a 24-atom chain with 6 PEG units, and the HAT inhibitor CPI-1612. This compound exhibits antiproliferative effects on multiple myeloma cells LP1 (DC50 = 1.2 μM), MM1S, and various cancer cells, notably leukemia cells.

QC-182 is a potent p300/CBP PROTAC degrader. It reduces p300 protein levels in SK-HEP-1 cells with a DC50 of 93 nM. QC-182 effectively inhibits cell growth in SK-HEP-1 and JHH7 cell lines, with IC50 values of 0.733 μM and 0.477 μM, respectively. QC-182 is applicable for hepatocellular carcinoma (HCC) research.

XYD198 (Compound 14h) is an orally active degrader of CBP/p300. It inhibits the CBP/p300 bromodomain with an IC50 of 213.5 nM and exhibits antitumor activity against acute myeloid leukemia.

XYD190 (Compound 14g) is an orally active degrader of CBP/p300. It inhibits the bromodomain of CBP/p300 with an IC50 of 483.7 nM and demonstrates antitumor activity against acute myeloid leukemia.

XYD129 is an effective CBP/p300 PROTAC degrader with antiproliferative activity, demonstrated by an IC50 of 0.044 μM against the MV4-11 cell line. It is applicable to research focusing on acute myeloid leukemia (AML).

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.