cbp

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.

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

Butyrolactone 3 (MB-3) is a histone acetyltransferase Gcn5 inhibitor with a weak affinity for CBP.Butyrolactone 3 has antimicrobial activity and has been used in cancer, metabolic and neurological disorders.

E-7386 is an oral active CBP -catenin modulator.

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 a selective ligand that binds to the target protein for PROTAC[dCBP-1], a potent and selective heterobifunctional degrader of p300 CBP.

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 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 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.

CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy.

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.

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

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-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-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.

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

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].

XDM-CBP is an effective and selective CBP/p300 bromodomain inhibitor.

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

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.

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).

CBP/p300-IN-14, efficiently inhibits CBP/EP300 (lysine acetyltransferase) with an IC50 value of 3.3 nM.

CBP-307 is a selective second generation S1P1 (a G-protein coupled receptor -GPCR) modulator.