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bromodomain

" in MedChemExpress (MCE) Product Catalog:

283

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13030
    (+)-JQ-1
    Maximum Cited Publications
    295 Publications Verification

    JQ1

    Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Neurological Disease Cancer
    (+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .
    (+)-JQ-1
  • HY-111784
    Inobrodib
    10+ Cited Publications

    CCS1477

    Epigenetic Reader Domain Cancer
    Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .
    Inobrodib
  • HY-78695
    JQ-1 carboxylic acid
    5+ Cited Publications

    Epigenetic Reader Domain PD-1/PD-L1 Ligands for Target Protein for PROTAC Cancer
    JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
    JQ-1 carboxylic acid
  • HY-13032
    Molibresib
    20+ Cited Publications

    I-BET762; GSK525762; GSK525762A

    Epigenetic Reader Domain Cancer
    Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
    Molibresib
  • HY-13235
    I-BET151
    25+ Cited Publications

    GSK1210151A

    Epigenetic Reader Domain Cancer
    I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively .
    I-BET151
  • HY-100015
    Mivebresib
    10+ Cited Publications

    ABBV-075

    Epigenetic Reader Domain Apoptosis Cancer
    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM .
    Mivebresib
  • HY-18975
    I-BRD9
    5+ Cited Publications

    Epigenetic Reader Domain Inflammation/Immunology Cancer
    I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC50 value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways .
    I-BRD9
  • HY-136521

    Epigenetic Reader Domain Cancer
    AZ13824374 is a potent and selective ATAD2 bromodomain inhibitor (pIC50 of 6.9 in HCT116 cells). AZ13824374 disrupts chromatin interactions and gene transcription by binding to the acetyl-lysine binding site of the ATAD2 bromodomain. AZ13824374 has anticancer activity against breast cancer .
    AZ13824374
  • HY-136938
    NEO2734
    4 Publications Verification

    EP31670

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains . NEO2734 is active in SPOP mutant and wild-type prostate cancer .
    NEO2734
  • HY-151594

    Epigenetic Reader Domain Inflammation/Immunology Cancer
    iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology .
    iBRD4-BD1
  • HY-134463
    NHWD-870
    1 Publications Verification

    Epigenetic Reader Domain Apoptosis Cancer
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
    NHWD-870
  • HY-40249

    Drug Intermediate Others
    1-Boc-1,2,3,6-tetrahydropyridine-4-boronic acid pinacol ester is a drug intermediate that can be used for the preparation of SMARCA bromodomain ligands .
    1-Boc-1,2,3,6-tetrahydropyridine-4-boronic acid pinacol ester
  • HY-145667
    Biotinylated-JQ1
    1 Publications Verification

    Biotin-JQ1

    Epigenetic Reader Domain Cancer
    Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM .
    Biotinylated-JQ1
  • HY-145550

    BI894999

    Epigenetic Reader Domain Cancer
    Amredobresib (BI894999) is an orally active BET inhibitor. Amredobresib inhibits the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer .
    Amredobresib
  • HY-100220
    GSK6853
    2 Publications Verification

    Epigenetic Reader Domain Cancer
    GSK6853, a chemical probe, is a potent and selective inhibitor of the BRPF1 bromodomain. GSK6853 shows excellent BRPF1 potency (pKd = 9.5) and greater than 1600-fold selectivity over all other bromodomains .
    GSK6853
  • HY-18665

    Epigenetic Reader Domain Cancer
    GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM .
    GSK-5959
  • HY-101088
    CeMMEC13
    1 Publications Verification

    DNA/RNA Synthesis Cancer
    CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 μM.
    CeMMEC13
  • HY-131061

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .
    BET bromodomain inhibitor 1
  • HY-103036

    Epigenetic Reader Domain Apoptosis Cancer
    BET bromodomain-IN-5 is an orally active BET inhibitor with an IC50 of 14 nM against BRD4 (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors .
    BET bromodomain-IN-5
  • HY-100729
    GSK9311
    1 Publications Verification

    Epigenetic Reader Domain Cancer
    GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively .
    GSK9311
  • HY-148116

    Epigenetic Reader Domain Cancer
    DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8 (1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki>1000 nM) .
    DN02
  • HY-19336
    BAZ2-ICR
    2 Publications Verification

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .
    BAZ2-ICR
  • HY-147868

    Epigenetic Reader Domain Apoptosis Cancer
    DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis .
    DC-CPin711
  • HY-19553

    Epigenetic Reader Domain Inflammation/Immunology
    LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells .
    LP99
  • HY-148739

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma .
    dBRD 9-A
  • HY-149026

    Epigenetic Reader Domain Others
    GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis .
    GNE-064
  • HY-100517
    TP-472
    2 Publications Verification

    Epigenetic Reader Domain Apoptosis Cancer
    TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7 . TP-472 induces apoptosis of melanoma cells .
    TP-472
  • HY-138563

    Epigenetic Reader Domain Cancer
    GSK973, a chemical probe, 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-146208
    BRD4 Inhibitor-20
    1 Publications Verification

    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-43723

    Ligands for Target Protein for PROTAC Cancer
    PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain .
    PROTAC BET-binding moiety 2
  • HY-110374
    NVS-CECR2-1
    1 Publications Verification

    Epigenetic Reader Domain Apoptosis Cancer
    NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism . NVS-CECR2-1 is a chemical probe.
    NVS-CECR2-1
  • HY-124596

    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-145125

    PROTACs Others
    SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.
    SJ995973
  • HY-W017851

    Drug Intermediate Neurological Disease
    4-Phenyl-2-pyrrolidinone is a precursor and synthetic intermediate. 4-Phenyl-2-pyrrolidinone can be used as a precursor in the synthesis of compounds with anticonvulsant and nootropic activities and is an intermediate in the synthesis of bromodomain-containing protein 4 (BRD4) bromodomain 1 inhibitors .
    4-Phenyl-2-pyrrolidinone
  • HY-111420

    Epigenetic Reader Domain Cancer
    CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.
    CBP/p300-IN-1
  • HY-139148

    Epigenetic Reader Domain Cancer
    UMB298 is a potent and selective CBP/P300 bromodomain inhibitor .
    UMB298
  • HY-170817

    Ligands for Target Protein for PROTAC SWI/SNF Complex Cancer
    SMI-1074, a SMARCA bromodomain inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMI-1074 can be used for synthesis SMD-3236 (HY-170824) and SMD-1087 (HY-170828). SMI-1074 can be used for the research of smarca4-deficient cancers .
    SMI-1074
  • HY-143332

    Epigenetic Reader Domain Cancer
    TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research .
    TRIM24/BRPF1-IN-2
  • HY-112149A

    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-151364

    HDAC Cancer
    HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
    HDAC6/8/BRPF1-IN-1
  • HY-177124

    VYN201

    Epigenetic Reader Domain Cancer
    Repibresib (VYN201) is a bromodomain and extra-terminal motif (BET) inhibitor. Repibresib shows antineoplastic activity .
    Repibresib
  • HY-145431

    Epigenetic Reader Domain Parasite Infection
    (S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .
    (S)-GSK1379725A
  • HY-123626

    Epigenetic Reader Domain Cancer
    BiBET is a chemical probe of BET/BRD4 and is able to bind to two bromodomains simultaneously in a bivalent and cis-binding mode .
    BiBET
  • HY-151528

    Epigenetic Reader Domain 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-1
  • HY-146445

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells .
    P300 bromodomain-IN-1
  • HY-116349

    Epigenetic Reader Domain Cancer
    Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 .
    Bromodomain IN-1
  • HY-135236

    Epigenetic Reader Domain Cancer
    OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity .
    OXFBD04
  • HY-19549

    Epigenetic Reader Domain Cancer
    RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki values of 3.2-24.7 nM. RX-37 can be used for research of cancers .
    RX-37
  • HY-150516S

    Epigenetic Reader Domain Cancer
    BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4 .
    BET-IN-12
  • HY-78197

    Drug Intermediate Others
    3,5-Dimethylisoxazole-4-boronic acid pinacol ester is a drug intermediate that can be used for the synthesis of bromodomain inhibitors .
    3,5-Dimethylisoxazole-4-boronic acid pinacol ester

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