cbp/ep300

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

CBP EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor targeting the bromodomain receptors of CBP EP300, demonstrating nanomolar-level binding affinity with proteins possessing bromodomains.

EP300 CBP-IN-1 (compound 172), a potent inhibitor of EP300 CBP, exhibits IC 50 values of 2.1 nM for EP300 BRD and 2.3 nM for CBP BRD. It effectively inhibits the proliferation of prostate cancer CWR22RV1 cells [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.

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.

JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.

SGC-CBP30 is an effective CREBBP EP300 inhibitor (IC50: 21 38 nM).

CPI-637 is a selective and cell-active benzodiazepinone CBP EP300 bromodomain inhibitor.

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.

GNE-272 is a selective inhibitor of CBP EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP EP300.

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.

CPI703 is a novel potent and specific CBP/EP300 bromodomain inhibitor.

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.

CPI-1612 is a potent, orally active EP300 CBP histone acetyltransferase (HAT) inhibitor that acts on EP300 HAT (IC50: 8.1 nM). CPI-1612 exhibits anticancer effects.

DS17701585 is an orally active, selective inhibitor of EP300 and CBP, capable of acting on CBP (IC50: 0.040 μM), EP300 (IC50: 0.15 μM), H3K27 (IC50: 0.45 μM) and SOX2 (IC50: 0.7 μM), and can be used to study cancer.

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.

DS-9300, an orally administered potent and selective inhibitor of EP300 CBP HAT, exhibits a significant inhibitory activity with an IC50 value of 28 nM. Demonstrating anticancer properties, it is utilized in research focused on prostate cancer disease.

PLX51107 is a potent and selective BET inhibitor with Kds of 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1, respectively.