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GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity .
PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer .
PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer .
PBRM1-BD2-IN-4 (compound 15) is a potent PBRM1 Bromodomain inhibitor with Kd values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.2 μM for PBRM1-BD2. PBRM1-BD2-IN-4 can be used to research anticancer .
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research .
BET BD2-IN-3 (compound I-58) is an inhibitor of BET, targeting the BD2 domain of BET. BET BD2-IN-3 can be radiolabeled with [11C] for positron emission tomography (PET) imaging. BET [11C]BD2-IN-3 showed suitable biodistribution in peripheral organs and tissues in PET applications in mice .
PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer .
PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer .
PBRM1-BD2-IN-6 is a potent PBRM1 bromodomain inhibitor with an IC50 value of 0.22 μM. PBRM1-BD2-IN-6 shows antiproliferation activity. PBRM1-BD2-IN-6 has the potential for the research of PBRM1-dependent cancer .
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media .
GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases .
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models [2].
GSK217
is a potent, selective, and highly soluble bromo and extraterminal domain (BET)
second bromodomain (BD2) inhibitor. GSK217 can be used for
the research of oncology and immune inflammation research .
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity .
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice .
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) .
SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2(BD2), BRD4 (BD1), and BRD4 (BD2) with IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively .
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .
PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases .
ZEN-2759 is a potent BET (Bromodomain and Extra-Terminal Domain) inhibitor, with IC50 values of 0.23, 0.08 and 0.28 μM for BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2), respectively .
BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4 BD2 in cells.
BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1) .
Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively .
ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC50 values of 0.64, 0.25 nM for BRD4-BD1, BRD4-BD2, respectively. BET-IN-15 shows antiproliferative activity .
GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4 .
ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4 .
ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .
MS417 is a selective BET-specific BRD4 inhibitor, binds to 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 (IC50, 32.7 μM).
Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro .
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively .
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer .
BRD4 Inhibitor-31 (Example 136) is a BRD4 inhibitor (Kis: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS .
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .
BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2(BD2) and BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research .
BET-IN-26 (compound 13a) is a potent, selective and orally active BD1 inhibitor with IC50 values of 0.0055, 9.0 µM for BD1, BD2, respectively. BET-IN-26 decreases LPS (HY-D1056) induced serum levels of IL-6 and MCP-1 .
PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .
BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC50 of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases .
GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer .
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
BRD4 degrader-3 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively . PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research .
BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC50 values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer .
(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .
BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
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 .
BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity .
SJ46421 is a (+)-JQ-1 (HY-13030) based KLHDC2-BRD3 PROTAC protein degrader. SJ46421 induces cooperative ternary complexes with KLHDC2 and BRD3BD2, with an IC50 of 7.8 nM. SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation. SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4. SJ46421 possesses poor cell permeability. (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-168536)) .
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells .
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
(2R,3R)-GSK973 is an isomer of GSK973. GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family .
BRD3 Protein, Human (BD2, GST) is the recombinant human-derived BRD3, expressed by E. coli , with N-GST labeled tag. The total length of BRD3 Protein, Human (BD2, GST) is 112 a.a.,
BRD3 Protein, Human (BD2, His) is the recombinant human-derived BRD3, expressed by E. coli , with N-6*His labeled tag. The total length of BRD3 Protein, Human (BD2, His) is 112 a.a.,
