brd-4

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

AW68 is a potential small molecule BRD4 inhibitor that prevents and treats BRD4-related diseases and can be used in cancer research.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

OXFBD04 is a potent and selective BRD4 inhibitor (IC50= 166 nM), a BET bromodomain ligand with modest affinity for the CREBBP bromodomain, and exhibits anti-cancer activity.

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

GNE-375 is a selective and potent BRD9 inhibitor (IC50: 5 nM).GNE-375 inhibits BRD4, TAF1, and CECR2, and can be used to study epigenetic resistance.

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.

CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).

3-methyl-1,2,3,4-tetrahydroquinazolin-2-one is a inhibitor of BRD4 .

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

FL-411 (BRD4-IN-1) is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4.

ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with nanomolar binding affinities to the bromodomains (BDs) of BRD4, exhibiting IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.

SRX3177 is a novel and potent inhibitor of BRD4, PI3K and CDK.SRX3177 has potential anticancer activity.

Tz-Thalidomide is a tetrazine-modified Thalidomide (E3 ligase ligand) with some affinity for BRD4.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor that inhibits BRD4 with an IC50 of 5193nM.

BRD4 Inhibitor-24 is a BRD4 small molecule inhibitor with antitumor activity.

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[1].

PROTAC BRD4 Degrader-5 is a PROTAC that efficiently degrades BRD4 in HER2-positive and -negative breast cancer cell lines, and is formed by linking von Hippel-Lindau ligand to BRD4 ligand.

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

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

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.

(Rac)-BAY1238097 is a inhibitor of BET(IC50 of 1.02 μM for BRD4),used in cancer research.