bromodomain

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

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.

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

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

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].

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).

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. It specifically inhibits BRD4 with an IC50 of 2.6 nM. Additionally, BET bromodomain inhibitor 1 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.

BET bromodomain inhibitor 2 is a potent inhibitor of the BET-type bromodomain (IC50: 14.1 μM).

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 IN-1 is an inhibitor of Bromodomain.

CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).

CHEMBRDG-BB 7118966 is an inhibitor of Bromodomain-containing protein 4 (human).

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

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.

3-methyl-1,2-dihydroquinolin-2-one is the first known micromolar inhibitors of the ATAD2 bromodomain.

GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].

1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one is an inhibitor Bromodomain-containing protein 4 (human).

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

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

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.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves 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). OXFBD04 is a potent BET bromodomain ligand and exhibits additional modest affinity for the CREBBP bromodomain. OXFBD04 exhibits anti-cancer 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, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity.

DN02 is a selective and efficient probe for the bromodomain of BRD8.DN02 has an affinity for BRD8 (1) and BRD8 (2).

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.

PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, demonstrating dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and boasts an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between the full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, which positions it as a promising candidate for anticancer research.

NEO2734 (EP31670) is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

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).

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

Hexamethylene bisacetamide inhibits BET Bromodomain Proteins.

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

I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.

Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.

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

GSK097 is a highly potent and selective inhibitor of the second bromodomain (BD2) found in bromodomain and extra-terminal domain (BET) proteins. It exhibits a remarkable 2000-fold selectivity for BD2 over BD1, as indicated by BRD4 data. Additionally, GSK097 demonstrates solubility of over 1 mg/mL in FaSSIF media.

A947, a potent and selective SMARCA2 proteolysis-targeting chimera (PROTAC) molecule, also acts as a moderately selective SMARCA2 degrader. It exhibits strong binding affinity to the SMARCA2 bromodomain, with a dissociation constant (K d) of 93 nM, making it a valuable tool for cancer research [1].

PROTAC BRD9 Degrader-5 is a proteolysis targeting chimera (PROTAC) designed for the specific degradation of Bromodomain-containing protein 9 (BRD9).

MMH2 is a novel molecular glue degrader targeting BRD4 by facilitating the recruitment of CUL4 and DCAF16 ligases to BRD4's second bromodomain (BRD4 BD2) [1].

Biotinylated-JQ1 (Biotin-JQ1), a biotinylated derivative of JQ1, selectively binds to the BRD4 bromodomain with high affinity. It effectively inhibits the proliferation of MM1.S multiple myeloma cells, demonstrating an EC50 of 0.4 μM [1].

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that facilitates the nuclear import of cytosolic cargoes by leveraging the nuclear-localized bromodomain-containing protein 4 (BRD4) as a carrier for their co-import and subsequent nuclear entrapment [1].

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

BRD7-IN-2 (compound 2-77) is a potent selective inhibitor of bromodomain-containing protein 7 (BRD7), exhibiting significant anti-proliferative activity in prostate cancer cells. It demonstrates an IC50 of 5.4 μM for BRD7 while showing weak inhibition for BRD9 with an IC50 of >300 μM.

MMH1, a novel molecular glue degrader of BRD4, operates by enlisting the CUL4 and DCAF16 ligases to target the second bromodomain (BRD4 BD2) [1].

GNE-235, a selective inhibitor of PBRM1's second bromodomain, exhibits a dissociation constant (K D) of 0.28 ± 0.02 μM, and can be utilized to assess the cellular function of PBRM1 [1].

Naringenin (NSC-11855) is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate metabolism promoter, immunity system modulater. This substance has also been shown to repair DNA.

(±)-Naringenin (Naringenine) is a natural product. It displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.