cbp 1

PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

Inobrodib (CBP-IN-1) is a potent inhibitor of p300/CBP bromodomain.

CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.

β-catenin/CBP-IN-1 is a potent and selective inhibitor of CBP/β-catenin

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

CBP-IN-1 (compound 12) is a potent CBP inhibitor with an IC50 of 1.5 nM, additionally suppressing CBP BRET and BRD4(1) with IC50 values of 690 nM and 3100 nM, respectively [1].

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

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

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.

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.

CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) with MMAE, targeting folate receptor (FRα) and TRPV6. It exhibits high binding affinity to FRα and low affinity to TRPV6. CBP-1008 shows antitumor activity and can be utilized for research in advanced solid tumors such as colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.

CBP-1018 is a peptide-drug conjugate (PDC) composed of a dual-targeting ligand for FRα/TRPV6, linked to Monomethylauristatin E. It holds promise for research in the field of breast cancer.

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione)  as a bona fide is a potent p300/CBP inhibitor

GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

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.

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.

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.

CBP/p300-IN-22 is a selective inhibitor of the CBP/EP300 bromodomain, with an IC50 of 4 nM. It exhibits high selectivity for BRD4(1) and reduces cytokine expression induced by TNF-α as well as subsequent immune cell recruitment by inhibiting NF-κB signaling, demonstrating anticancer properties. This compound is applicable for research into rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory diseases.

IQ 1 has multiple roles, such as maintaining the multifunctionality of mouse ESCs, decreasing Wnt-stimulated phosphorylation, blocking PP2A/Nkd interactions, and so on.

CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains, inhibiting CBP with an IC50 range of 0.01-0.1 μM and BRD4 with an IC50 range of 1-1000 μM.