cbp/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.

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

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

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.

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.

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.

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

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).

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.

ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

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.