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.

I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).

The S-enantiomer of BET-BAY 002, referred to as BET-BAY 002 S enantiomer, is a potent inhibitor of BET (Bromodomain and Extra-Terminal motif proteins).

BET-BAY 002 is an effective BET bromodomain inhibitor demonstrating efficacy in vivo and in vitro against multiple myeloma and leukaemia models.

BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.

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 a carboxylic acid derivative of I-BET762, a ligand that specifically targets BET, and is primarily used in the synthesis of PROTAC molecules. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 of 5.1.

BET bromodomain inhibitor is a potent BET inhibitor.

I-BET 151 dihydrochloride is a BET bromodomain inhibitor that prevents BET from recruiting to chromatin.

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.

BET bromodomain inhibitor 1 is an orally active, selective inhibitor of bromodomain and extra-terminal (BET) proteins, specifically inhibiting BRD4 with an IC50 of 2.6 nM. It also demonstrates high affinities towards BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, and 2.1 nM, respectively. This compound exhibits anti-cancer activity.

I-BET469 is a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose.

I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1].

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.

ODM-207 (BET-IN-4) is a potent inhibitor of BRD4.

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

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.

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

ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.