p300/cbp

CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.

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.

CBP/p300 ligand 3, a specific target protein ligand of CBPD-268, modulates the function of CBP and p300. These two proteins, which possess histone acetyltransferase (HAT) activity, are crucial in the regulation of gene expression, cell proliferation, differentiation, and DNA repair by acetylating histones and other proteins. This ligand operates by binding to a particular domain within the CBP/p300 proteins (the bromine domain or HAT domain), either inhibiting their enzymatic activity or altering their interactions with other proteins (transcription factors). CBP/p300 ligand 3 is applicable in research on cancer, neurodegenerative diseases, and other conditions marked by abnormal CBP/p300 activity.

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.

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

NEO2734 (EP31670) is an orally active, selective inhibitor of p300/CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.

P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).

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.

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 of 15.9 μM against recombinant HAT p300/CBP-associated factor (PCAF) and exhibits anti-proliferative activity against certain cancer cells, making it useful for anti-cancer research.

A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.

Piflufolastat (DCFPYL) is a PET imaging agent for prostate cancer PSMA. It is a fluorinated prostate-specific membrane antigen (PSMA) preparation. Piflufolastat can be used to prepare piflufolastat F 18 (DCFPyL F-18).

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor that inhibits BRD4 with an IC50 of 5193nM.

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

C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.

CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM for CBP/HTRF and 5.96 nM for Myc.