p300/cbp

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

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.

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).

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.

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.

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-IN-14, efficiently inhibits CBP/EP300 (lysine acetyltransferase) with an IC50 value of 3.3 nM.

CBP/p300-IN-17 (compound 7) is a potent inhibitor of EP300/CBP HAT, with an IC50 of 0.18 μM for HAT EP300 and 0.69 μM for LK2 H3K27.

CBP/p300-IN-16 (compound 1) is a potent inhibitor of EP300/CBP HAT, targeting HAT EP300 with an IC50 of 0.61 μM and LK2 H3K27 with an IC50 of 2.24 μM.

CBP/p300-IN-18 (compound 8) is a potent inhibitor of EP300/CBP HAT, with an IC50 of 0.056 μM for HAT EP300 and 0.46 μM for LK2 H3K27.

CBP/p300-IN-15 (compound 13a) is a potent inhibitor of p300 (IC50: 2.5 nM) and CBP (IC50: 28.0 nM). It inhibits OVCAR-3 cells (EC50: 0.865 μM) and A2780 cells (EC50: 2.71 μM). CBP/p300-IN-15 can be used to study ovarian cancer.

CBP/p300-IN-19 is a potent inhibitor of p300/CBP HAT, effective against P300-HAT (IC50: 1.4 μM), CBP-HAT (IC50: 1.4 μm, 2.2 μM), PCAF (IC50: >100 μM), and Myst3 (IC50: >100 μM), demonstrating anti-tumor activity.

CBP/p300-IN-19 hydrochloride is a selective and potent inhibitor of p300/CBP HAT, with IC50 values of 1.4 μM for p300-HAT, 2.2 μM for CBP-HAT, and over 100 μM for both PCAF and Myst3, and has antitumor effects.

CBP/p300-IN-10, a potent inhibitor targeting histone acetyltransferase enzymes EP300 and CREBBP, exhibits IC50 values of 26 nM and 39 nM, respectively. This compound shows potential for anticancer research applications.

CBP/p300-IN-21 (Compound 5d) is a selective inhibitor of CBP/p300, with IC50 values of 0.07 μM for p300 and 1.755 μM for CBP; it reduces H3K18Ac levels and inhibits the growth of 4T1 tumors in mice [1].

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.