bet

PROTAC BET Degrader-1 is a potent BET degrader utilizing the PROTAC mechanism.

PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.

BET-IN-6, a ligand with potent and high affinity for inhibiting BRD2/BRD4, plays a crucial role in the synthesis of PROTAC BRD2/BRD4 degrader-1 [1], targeting the protein BRD2/4.

PROTAC BET-binding moiety 1 is a crucial intermediate used in synthesizing high-affinity BET inhibitors.

PROTAC BET-binding moiety 2 is an inhibitor of the BET bromodomain.

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins, with an IC50 of 9.6 nM.

I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).

PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM.

dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis.

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

Thalidomide-O-C6-NH2 hydrochloride (4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride) is a synthesized E3 ligase ligand-linker conjugate.

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising an (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.

(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) is a synthesized E3 ligase ligand-linker conjugate, incorporating an (S,R,S)-AHPC-based VHL ligand and a linker[1].

ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.

AR/BET protein degrader-1 (Compound 149) is a dual-targeting protein degrader of Androgen Receptor and BET (bromodomain and extra-terminal domain), suitable for cancer research.

PROTACBET Degrader-12 (Compound 8b) is a PROTAC degrader targeting proteins with bromodomains and extraterminal (BET) domains, facilitating the degradation of BRD3 and BRD4 in a DCAF11-dependent manner. It inhibits the viability of KBM7 cells with a DC50 of 305.2 nM.

PROTACBET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader that targets BET proteins. It effectively degrades the PML-eGFP-BRD4 fusion protein, causing a near-complete loss of EGFP+ nuclear foci with an EC50 of 1.4 μM.

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

Azido-PEG4-beta-D-glucose is a polyethylene glycol (PEG)-based linker compound crucial for the efficient synthesis of proteolysis targeting chimeras (PROTACs)[1].

Azido-PEG4-tetra-Ac-beta-D-glucose is a polyethylene glycol (PEG)-based PROTAC linker used for PROTAC synthesis[1].

Propargyl-PEG4-beta-D-glucose is a polyethylene glycol (PEG) derivatized PROTAC linker used in the synthesis of PROteolysis TArgeting Chimeras (PROTACs)[1].