bromodomain

LP99 is an epigenetic probe. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. LP99 is an effective and selective inhibitor of the BRD7 and BRD9 bromodomains (Kd: 99 nM against BRD9).

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

Bromodomain IN-1 is an inhibitor of Bromodomain.

Bromodomain inhibitor-8 is an inhibitor of BET bromodomain used to treat autoimmune and inflammatory diseases.

Bromodomain Inhibitor-13 (Compound 1), an analog of PFI-3, is a bromodomain-containing protein (BCP) inhibitor. It specifically targets the bromodomains of SMARCA2, SMARCA4, and the first and second bromodomains of PB1 [PB1(5) and PB1(2)], with dissociation constants (KD) of 37, 53, 30, and 190 nM, respectively.

BET bromodomain inhibitor is a potent BET inhibitor.

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.

Bromodomain inhibitor-10 (compound 128) is a highly potent bromodomain activity inhibitor, exhibiting strong binding affinity with Kd values of 15.0 nM and 2500 nM for BRD4-1 and BRD4-2, respectively. It also effectively inhibits the production of IL12p40 [1].

BET bromodomain inhibitor 2 is a potent inhibitor of the BET-type bromodomain with an IC50 of 14.1 μM.

Bromodomain inhibitor-9 is an inhibitor of Bromodomains that selectively inhibits the activity of BRD4-1 with a Kd value of 12 nM. Bromodomain inhibitor-9 can be used in studies of diseases related to systemic or lipid metabolism, tissue inflammation, fibrosis, or chronic autoimmune diseases.

P300 bromodomain-IN-1 is a potent inhibitor of p300 (EP300) bromodomain (IC50: 49 nM). p300 bromodomain-IN-1 blocks c-Myc expression and induces cell cycle arrest at G1 G0 phase and apoptosis in OPM-2 cells. apoptosis).

BD-IN-1, a pan bromodomain (BD) inhibitor, exhibits K_D values of 250 nM for BRD4(1), 420 nM for CBP, 130 nM for BRPF1B, 430 nM for BRD7, 67 nM for BRD9, 240 nM for BRDT(1), and 970 nM for CECR2, respectively. This compound demonstrates antiproliferative activity [1].

BET Bromodomain Inhibitor 3 is a BET bromodomain inhibitor with an inhibitory Ki value of >40 µM against BrdT. It is utilized in research related to contraception, cancer, and heart disease [1].

Bromodomain Inhibitor-12 (example 303) is a research compound utilized in the study of autoimmune and inflammatory diseases [1].

Bromodomain Inhibitor-12 Edisylate (example 303) serves as a bromodomain inhibitor applicable to autoimmune and inflammatory disease research [1].

BET bromodomain inhibitor 4 (example 7) acts as an inhibitor of the BET bromodomain domain [1].

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.

Inobrodib (CBP-IN-1) is a potent inhibitor of p300 CBP bromodomain.

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

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.

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

FT001 is a potent, selective and orally available inhibitor of BET Bromodomain with antitumor activity. FT001 inhibited the expression of MYC with the IC50 value of 0.46 μM). FT001 has potent antiproliferative effects against MV-4-11 and demonstrates significant MYC mRNA suppression both in vitro and in vivo.