bet bromodomain inhibitor 1

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.

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.

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.

Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).

(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1, a BET bromodomain inhibitor, which acts on BRD4(1/2) with IC50 values of 77 nM and 33 nM in a cell-free assay.

XD14 is an inhibitor of BET bromodomain (Kd of 160 nM, 170 nM, 380 nM, 490 nM, 830 nM and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2), respectively).

(+)-JQ1-OH is the primary metabolite of (+)-JQ1. (+)-JQ-1 (JQ1) is a potent, specific, and reversible inhibitor of BET bromodomain, with IC50 values of 77 nM for the first bromodomain and 33 nM for the second bromodomain (BRD4(1/2)). Additionally, (+)-JQ-1 stimulates autophagy (autophagy).

BET-IN-18 (Compound 3) is a broad-spectrum BET bromodomain small-molecule inhibitor with Ki values of 0.69 μM and 0.37 μM for BrdT(1) and Brd4(1) bromodomains, respectively, and Kd values of 1.6 μM and 8.4 μM. This compound effectively competes with the known BET inhibitor (+)-JQ1 for binding to Brd4(1) and BrdT(1), with IC50 values of 1.0 μM and 2.3 μM, respectively. Additionally, BET-IN-18 competitively inhibits the binding of acetylated histone substrates to Brd4(1) (IC50 = 0.90 μM). It is applicable in the study of multiple myeloma.

INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM respectively.

RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell

TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020)

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+)-JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.

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.

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

NVS-BET-1 is a BET bromodomain inhibitor that can regulate keratinocyte plasticity.

PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.

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

(+)-JQ-1 carboxylic acid is a potent bromodomain and extra terminal domain (BET) inhibitor. (+)-JQ-1 carboxylic has potential to be used as a precursor to synthesize PROTACs and other conjugates.

NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor with significant affinity for various BRD4 and BRDT isoforms, as demonstrated by its Kd values of 0.095 nM for BRD4-1, 0.32 nM for BRD4-2, 0.29 nM for BRD4-T, 0.089 nM for BRDT-1, 5.5 nM for BRDT-2, and 0.058 nM for BRDT-T. Additionally, NC-III-49-1 exhibits antiproliferative effects and reduces the expression of c-Myc [1].

GXH-II-052 is a potent bivalent inhibitor targeting the bromodomain and extraterminal domain (BET), exhibiting significant binding affinity to various BET proteins, including BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, and BRDT-T, with dissociation constants (Kd) of 28, 9.1, 4.8, 0.6, 8.4, and 2.6 nM, respectively. Additionally, GXH-II-052 demonstrates antiproliferative effects and reduces the expression of c-Myc [1].

BET-IN-16 (Comp I), a bromodomain and extra-terminal (BET) inhibitor, demonstrates anticancer activity by impeding the growth of prostate cancer cells. It exhibits potent inhibitory effects with half-maximal inhibitory concentration (IC50) values of 0.043 μM for LNCaP cells and 0.034 μM for 22Rv1 cells [1].

GSK217 is a potent and selective inhibitor of the bromo and extraterminal domain (BET) second bromodomain (BD2) with high solubility, utilized in oncology and immune inflammation research [1].

BET bromodomain inhibitor 3 is a BET inhibitor with activity against BrdT (Ki > 40 μM). It serves as a chemical probe for studying epigenetic regulation in contraception and cancer research.

EBET-1055 is a degrader of bromodomain and extra-terminal (BET) proteins, consisting of a BET inhibitor (EBET-590), an E3 ubiquitin ligase ligand, and connectors. It effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC) and also modulates cancer-associated fibroblast (CAF) activity, enhancing all reporter gene activities in organoid co-cultures [1].