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BRD4 BD-2

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65

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111433
    BRD4 degrader AT1
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    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 degrader AT1
  • HY-111977
    ZEN-3219

    		Epigenetic Reader Domain Cancer
    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-3219
  • HY-129201
    ZEN-2759

    		Epigenetic Reader Domain Cancer
    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 .
    ZEN-2759
  • HY-138563
    GSK973

    		Epigenetic Reader Domain Cancer
    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 BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
    GSK973
  • HY-112149
    ZL0420

    		Epigenetic Reader Domain Inflammation/Immunology
    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.
    ZL0420
  • HY-147573
    BRD4 Inhibitor-23

    		Epigenetic Reader Domain Cancer
    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) .
    BRD4 Inhibitor-23
  • HY-142675
    BRD4-BD1/2-IN-2

    		Epigenetic Reader Domain Cancer
    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) .
    BRD4-BD1/2-IN-2
  • HY-142674
    BRD4-BD1/2-IN-1

    		Epigenetic Reader Domain Cancer
    BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5) .
    BRD4-BD1/2-IN-1
  • HY-111979
    ZEN-3411

    		Epigenetic Reader Domain Cancer
    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-3411
  • HY-170380
    XY221

    		Epigenetic Reader Domain Apoptosis AMPK c-Myc PAK Bcl-2 Family Cancer
    XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
    XY221
  • HY-155078
    BRD4 Inhibitor-27

    		Epigenetic Reader Domain 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-27
  • HY-111978
    ZEN-3862

    		Epigenetic Reader Domain Cancer
    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 .
    ZEN-3862
  • HY-176035
    MS479

    		PROTACs Epigenetic Reader Domain Cancer
    MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038) .
    MS479
  • HY-111139
    MS417
    4 Publications Verification

    GTPL7512

    		 Epigenetic Reader Domain HIV Infection Inflammation/Immunology
    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).
    MS417
  • HY-125232
    MS645

    		Epigenetic Reader Domain Cancer
    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 .
    MS645
  • HY-160634
    BRD4 Inhibitor-31

    		Epigenetic Reader Domain Infection Inflammation/Immunology 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 .
    BRD4 Inhibitor-31
  • HY-120000
    MS402
    1 Publications Verification

    		 Epigenetic Reader Domain Inflammation/Immunology Cancer
    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 .
    MS402
  • HY-16954
    ARV-825
    Maximum Cited Publications
    21 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
    ARV-825
  • HY-149098
    SJ1461

    		Epigenetic Reader Domain Cancer
    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 .
    SJ1461
  • HY-143317
    XY153

    		Epigenetic Reader Domain Cancer
    XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 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 .
    XY153
  • HY-173062
    BRD4 Inhibitor-40

    		Epigenetic Reader Domain c-Myc Others
    BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models .
    BRD4 Inhibitor-40
  • HY-152209
    BRD4 Inhibitor-26

    		Epigenetic Reader Domain Cancer
    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 .
    BRD4 Inhibitor-26
  • HY-153945
    BET-IN-15

    		Epigenetic Reader Domain Cancer
    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 .
    BET-IN-15
  • HY-136857
    BRD4 degrader-3

    		Epigenetic Reader Domain Cancer
    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.
    BRD4 degrader-3
  • HY-138555
    PROTAC BRD4 Degrader-8

    		PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-8
  • HY-138637
    PROTAC BRD4 Degrader-14

    		PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-14
  • HY-139294
    PROTAC BRD4 Degrader-15

    		PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-15
  • HY-143300
    BRD4-BD1-IN-2

    		Epigenetic Reader Domain Cardiovascular Disease Cancer
    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 .
    BRD4-BD1-IN-2
  • HY-173237
    CDK4/6/BRD4-IN-1

    		CDK Epigenetic Reader Domain Cancer
    CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC50 values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis .
    CDK4/6/BRD4-IN-1
  • HY-170686
    BRD4 Inhibitor-38

    		Interleukin Related TNF Receptor Epigenetic Reader Domain Inflammation/Immunology
    BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of BRD4 with IC50 values of 3.64 μM and 0.12 μM against BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC50 value of 1.98 μM for inhibiting nitric oxide (NO) production .
    BRD4 Inhibitor-38
  • HY-151972
    BRD4 Inhibitor-25

    		Epigenetic Reader Domain Cardiovascular Disease Inflammation/Immunology Cancer
    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.
    BRD4 Inhibitor-25
  • HY-146208
    BRD4 Inhibitor-20

    		Epigenetic Reader Domain Cancer
    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-20
  • HY-143327
    PROTAC BRD4 Degrader-16

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells .
    PROTAC BRD4 Degrader-16
  • HY-136571
    GSK046
    3 Publications Verification

    iBET-BD2

    		 Epigenetic Reader Domain Inflammation/Immunology
    GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity .
    GSK046
  • HY-143328
    PROTAC BRD4 Degrader-17

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells .
    PROTAC BRD4 Degrader-17
  • HY-112150
    ZL0454

    		Epigenetic Reader Domain Inflammation/Immunology
    ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
    ZL0454
  • HY-112376
    MZP-54
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4 BD2.
    MZP-54
  • HY-112377
    MZP-55
    1 Publications Verification

    		 Epigenetic Reader Domain PROTACs Cancer
    MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4 BD2.
    MZP-55
  • HY-112149A
    (E/Z)-ZL0420

    		Epigenetic Reader Domain Inflammation/Immunology Cancer
    (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 .
    (E/Z)-ZL0420
  • HY-126325
    BY27

    		Epigenetic Reader Domain Cancer
    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 .
    BY27
  • HY-149519
    BRD4 Inhibitor-28

    		Epigenetic Reader Domain Cancer
    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 .
    BRD4 Inhibitor-28
  • HY-124596
    CD161

    		Epigenetic Reader Domain Cancer
    CD161 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 .
    CD161
  • HY-114504
    RVX-297

    		Epigenetic Reader Domain Inflammation/Immunology
    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].
    RVX-297
  • HY-112429
    HJB97
    2 Publications Verification

    		 Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 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).
    HJB97
  • HY-132232
    GSK097

    		Epigenetic Reader Domain 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 .
    GSK097
  • HY-153241
    GSK737

    		Epigenetic Reader Domain Cancer
    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 .
    GSK737
  • HY-130622
    LT052

    		Epigenetic Reader Domain Inflammation/Immunology
    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 .
    LT052
  • HY-168628
    BET-IN-27

    		Epigenetic Reader Domain Cancer
    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 .
    BET-IN-27
  • HY-129937
    (S)-GNE-987

    		PROTACs Epigenetic Reader Domain 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) .
    (S)-GNE-987
  • HY-153894
    SRX3177

    		CDK Epigenetic Reader Domain PI3K Cancer
    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 .
    SRX3177

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