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Results for "

Bromodomains Inhibitors

" in MedChemExpress (MCE) Product Catalog:

142

Inhibitors & Agonists

1

Isotope-Labeled Compounds

2

Click Chemistry

Cat. No. Product Name Target Research Areas
  • HY-43723
    PROTAC BET-binding moiety 2

    		Ligands for Target Protein for PROTAC Cancer
    PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.
  • HY-146709
    BET bromodomain inhibitor 2

    		Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC50 of 14.1 µM.
  • HY-150516S
    BET-IN-12

    		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[1].
  • HY-146445
    P300 bromodomain-IN-1

    		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.
  • HY-153593
    BET bromodomain inhibitor 3

    		Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
  • HY-128703
    Bromodomain inhibitor-8

    		Epigenetic Reader Domain Inflammation/Immunology
    Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.
  • HY-153668
    Bromodomain inhibitor-12

    		Epigenetic Reader Domain Inflammation/Immunology
    Bromodomain inhibitor-12 (example 303) is a bromodomain inhibitor that can be used in the research of autoimmune and inflammatory diseases.
  • HY-147374
    Bromodomain inhibitor-9

    		Epigenetic Reader Domain Metabolic Disease Inflammation/Immunology
    Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases.
  • HY-153668A
    Bromodomain inhibitor-12 (edisylate)

    		Epigenetic Reader Domain Inflammation/Immunology
    Bromodomain inhibitor-12 edisylate (example 303) is a bromodomain inhibitor that can be used in the research of autoimmune and inflammatory diseases.
  • HY-19999
    PF-CBP1

    		Epigenetic Reader Domain Neurological Disease
    PF-CBP1 is a highly selective inhibitor of the CREB binding protein bromodomain.
  • HY-147375
    Bromodomain inhibitor-10

    		Epigenetic Reader Domain Cancer
    Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40.
  • HY-131061
    BET bromodomain inhibitor 1

    		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.
  • HY-116349
    Bromodomain IN-1

    		Epigenetic Reader Domain Cancer
    Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 .
  • HY-117286
    (S)-JQ-35

    TEN-010

    		 Epigenetic Reader Domain Cancer
    (S)-JQ-35 (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.
  • HY-100015
    Mivebresib
    5+ 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.
  • HY-157134
    Y08262

    		Others Cancer
    Y08262 is a potent and selective CBP bromodomain inhibitor. Y08262 selectively inhibits the CBP bromodomain with an IC50 value of 73.1 nM. Y08262 can be used for the research of acute myeloid leukemia (AML).
  • HY-145431
    (S)-GSK1379725A

    		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.
  • HY-100220
    GSK6853

    		Epigenetic Reader Domain Cancer
    GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain.
  • HY-136938
    NEO2734

    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.
  • HY-135236
    OXFBD04

    		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.
  • HY-142265
    NVS-BET-1

    		Epigenetic Reader Domain Others
    NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity.
  • HY-139148
    UMB298

    		Epigenetic Reader Domain Cancer
    UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.
  • HY-13030
    (+)-JQ-1
    Maximum Cited Publications
    187 Publications Verification

    JQ1

    		 Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, 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.
  • 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.
  • HY-15846A
    (Rac)-CPI-203

    		Others Cancer
    (Rac)-CPI-203 is a racemate of CPI-203 (HY-15846) (BET bromodomain inhibitor)
  • HY-142743
    Y08175

    		Epigenetic Reader Domain Cancer
    Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer.
  • HY-141843
    BRD4-IN-2

    		Epigenetic Reader Domain Inflammation/Immunology
    BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC50 value of 9.9 nM.
  • 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.
  • HY-115926
    BRD4 Inhibitor-16

    		Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information.
  • HY-111420
    CBP/p300-IN-1

    		Epigenetic Reader Domain Cancer
    CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.
  • HY-12409
    PFI-3
    3 Publications Verification

    		 Epigenetic Reader Domain Cancer
    PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
  • HY-149026
    GNE-064

    		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.
  • HY-128977
    CD235

    		Epigenetic Reader Domain Cancer
    CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor.
  • HY-13032
    Molibresib
    15+ 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.
  • HY-103036
    BET bromodomain inhibitor

    		Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
  • HY-124596
    CD161

    NKR-P1A

    		 Epigenetic Reader Domain Cancer
    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.
  • HY-18665
    GSK-5959

    		Epigenetic Reader Domain Cancer
    GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.
  • HY-151594
    iBRD4-BD1

    		Epigenetic Reader Domain Cancer Inflammation/Immunology
    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.
  • HY-151894
    I-BET432

    		Epigenetic Reader Domain Cancer
    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.
  • HY-147869
    DC-CPin7

    		Epigenetic Reader Domain Cancer
    DC-CPin7 is a potent inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 2.5 μM.
  • HY-13032B
    Molibresib besylate
    15+ Cited Publications

    GSK 525762C; I-BET 762 besylate

    		 Epigenetic Reader Domain Cancer
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-134463
    NHWD-870

    		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.
  • HY-141546
    Pocenbrodib

    		Histone Acetyltransferase Cancer
    Pocenbrodib (compound II) is a CBP/p300 family of bromodomain inhibitor. Pocenbrodib has the potential for cancer research.
  • HY-111916
    ODM-207

    BET-IN-4

    		 Epigenetic Reader Domain Cancer
    ODM-207 (BET-IN-4) is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ≤ 1 μM.
  • 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.
  • HY-16586
    PFI-1
    2 Publications Verification

    		 Epigenetic Reader Domain Autophagy Apoptosis Cancer
    PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.
  • HY-15743
    Birabresib
    20+ Cited Publications

    OTX-015; MK-8628

    		 Epigenetic Reader Domain Cancer
    Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
  • HY-103297
    OXFBD02

    		Epigenetic Reader Domain Cancer
    OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM.
  • HY-100697
    TPOP146
    2 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
  • HY-19541A
    I-CBP112 hydrochloride

    		Epigenetic Reader Domain Cancer
    I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
  • HY-107477
    GSK8573

    		Epigenetic Reader Domain Cancer
    GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments.
  • HY-115867
    GSK852

    		Epigenetic Reader Domain Cancer
    GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC50 = 7.9).
  • HY-15846
    CPI-203
    4 Publications Verification

    		 Epigenetic Reader Domain Apoptosis Cancer
    CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
  • HY-19541
    I-CBP112
    2 Publications Verification

    		 Histone Acetyltransferase Epigenetic Reader Domain Cancer
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
  • HY-111502
    Y06036

    		Epigenetic Reader Domain Cancer
    Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.
  • HY-115568
    BETd-246
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
  • HY-111503
    Y06137

    		Epigenetic Reader Domain Cancer
    Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
  • HY-12518
    OF-1
    3 Publications Verification

    		 Epigenetic Reader Domain Cancer
    OF-1 is a potent pan-BRPF bromodomain (BRD) inhibitor, with IC50 values of 270 nM, 1.2 μM for TRIM24 and BRPF1B, respectively.
  • HY-15826
    SGC-CBP30
    5+ Cited Publications

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer Inflammation/Immunology
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
  • HY-107424
    BAY-299
    2 Publications Verification

    		 Epigenetic Reader Domain Cancer
    BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
  • HY-13959
    MS436
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
  • 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.
  • HY-110106
    I-BET151 dihydrochloride

    GSK1210151A dihydrochloride

    		 Epigenetic Reader Domain Cancer
    I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
  • HY-13235
    I-BET151
    20+ 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.
  • HY-153242
    GSK217

    		Epigenetic Reader Domain Inflammation/Immunology
    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.
  • HY-16652
    Apabetalone
    5+ Cited Publications

    RVX-208; RVX000222

    		 Epigenetic Reader Domain HIV Cancer
    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.
  • HY-141890
    BAZ1A-IN-1

    		Epigenetic Reader Domain Cancer
    BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.
  • HY-19760
    I-BET282

    		Epigenetic Reader Domain Inflammation/Immunology
    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).
  • HY-141703
    DC-BPi-11

    		Epigenetic Reader Domain Cancer
    DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation.
  • HY-101125
    L-Moses
    2 Publications Verification

    L-45

    		 Epigenetic Reader Domain Cancer
    L-Moses (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
  • HY-101125A
    L-Moses dihydrochloride

    L-45 dihydrochloride

    		 Epigenetic Reader Domain Cancer
    L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
  • HY-141703A
    DC-BPi-11 hydrochloride

    		Epigenetic Reader Domain Cancer
    DC-BPi-11 hydrochloride is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 hydrochloride shows remarkable inhibition against leukemia cell proliferation.
  • HY-19537
    NI-57

    		Epigenetic Reader Domain Cancer Inflammation/Immunology
    NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.
  • HY-19553
    LP99

    		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.
  • HY-156814
    HPP-9

    		Hedgehog Cancer
    HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC50 of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity[1[.
  • HY-19336
    BAZ2-ICR
    1 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.
  • HY-19760B
    I-BET282E

    		Epigenetic Reader Domain Inflammation/Immunology
    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).
  • HY-117997
    UMB-32

    		Epigenetic Reader Domain Cancer
    UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor.
  • HY-128597
    BRD-IN-3

    		Epigenetic Reader Domain Cancer
    BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ.
  • HY-78695
    JQ-1 (carboxylic acid)
    3 Publications Verification

    		 Epigenetic Reader Domain PD-1/PD-L1 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.
  • HY-100729A
    GSK9311 hydrochloride

    		Epigenetic Reader Domain Cancer
    GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
  • HY-147868
    DC-CPin711

    		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.
  • HY-100729
    GSK9311

    		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.
  • HY-19999A
    PF-CBP1 hydrochloride
    1 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Neurological Disease
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
  • HY-100653
    AZD5153

    		Others Cancer
    AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors .
  • HY-15743A
    (R)-Birabresib

    (R)-OTX-015; (R)-MK-8628

    		 Others Cancer
    (R)-Birabresib is the inactive isomer of Birabresib (HY-15743), and can be used as an experimental control. Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
  • HY-114416
    GS-626510

    		Epigenetic Reader Domain Cancer
    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.
  • HY-149421
    BRD7-IN-3

    		Epigenetic Reader Domain Cancer
    BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7/BRD9 with IC50s of 1.6 μM and 2.7 μM respectively.
  • HY-19549
    RX-37

    		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.
  • HY-142772
    Y08284

    		Epigenetic Reader Domain Cancer
    Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.
  • HY-112789
    (+)-JQ1 PA
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • 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.
  • HY-117865
    GNE-886

    		Epigenetic Reader Domain Cancer
    GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM.
  • HY-145550
    Amredobresib

    BI894999

    		 Epigenetic Reader Domain Cancer
    Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1).
  • HY-100653A
    AZD5153 6-Hydroxy-2-naphthoic acid

    		Epigenetic Reader Domain Cancer
    AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
  • HY-109050
    Alobresib
    1 Publications Verification

    GS-5829

    		 Epigenetic Reader Domain Cancer
    Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.
  • HY-136521
    AZ13824374

    		Epigenetic Reader Domain Cancer
    AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively.
  • HY-100352
    BI-9564
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family.
  • HY-136920
    CBP/p300-IN-8
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC50=0.01-0.1 µΜ) and BRD4 (IC50=1-1000 µΜ) activity.
  • HY-145667
    Biotinylated-JQ1

    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.
  • HY-15658
    GSK2801
    2 Publications Verification

    		 Epigenetic Reader Domain Apoptosis Cancer
    GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
  • HY-100482
    CPI-637
    5+ Cited Publications

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.
  • HY-149420
    BRD7-IN-2

    		Epigenetic Reader Domain Others
    BRD7-IN-2 (compound 2-77) is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. BRD7-IN-2 is selective for BRD7 rather than BRD9, with IC50s of 5.4 μM, and >300 μM, respectively.
  • HY-149806
    Bromodomain IN-2

    		Epigenetic Reader Domain Cancer
    BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity.
  • 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.
  • HY-155889
    IV-275

    		Epigenetic Reader Domain Cancer
    IV-275 is an inhibitor of both BRG1 and BRM bromodomains. IV-275 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-275 inhibits the invasiveness of GBM cells. IV-275 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide.
  • HY-155888
    IV-255

    		Epigenetic Reader Domain Cancer
    IV-255 is a selective small molecule inhibitor of the BRG1 bromodomain. IV-255 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-255 inhibits the invasiveness of GBM cells. IV-255 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide.
  • HY-120028
    GNE-207

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
  • HY-18664
    PFI-4
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC50 of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions.
  • HY-136570
    GSK778

    iBET-BD1

    		 Epigenetic Reader Domain Apoptosis Cancer Inflammation/Immunology
    GSK778 (iBET-BD1) 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 phenocopies the effects of pan-BET inhibitors in cancer models.
  • 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.
  • HY-112149A
    (E/Z)-ZL0420

    		Epigenetic Reader Domain Cancer Inflammation/Immunology
    (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.
  • HY-119490
    UMB-136

    		Epigenetic Reader Domain HIV Infection
    UMB-136 is a bromodomain inhibitor. UMB-136 is a promising latency-reversing agent (LRA) for HIV-1 eradication. UMB-136 reactivates HIV-1 in multiple cell models. UMB-136 enhances HIV-1 transcription and increases viral production through the release of P-TEFb.
  • HY-153367
    FHD-609

    		Epigenetic Reader Domain Cancer
    FHD-609 is an inhibitor and a degrader of BRD9 (bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment.
  • HY-111422
    PLX51107
    3 Publications Verification

    		 Epigenetic Reader Domain Cancer
    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).
  • HY-125236
    BET-IN-19

    		Epigenetic Reader Domain Cancer
    BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 inhibits hlL-6 mRNA transcription (IC50 ≤ 0.3 uM), and c-myc activity in human AML MV4-11 cell (IC50 ≤ 0.3 uM)。BET-IN-19 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC50 ≤ 0.3 uM).
  • HY-100517
    TP-472

    		Epigenetic Reader Domain Apoptosis Cancer
    TP-472 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.
  • 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.
  • HY-136571
    GSK046
    2 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.
  • HY-137892
    GSK620

    		Epigenetic Reader Domain Inflammation/Immunology
    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.
  • HY-111784
    Inobrodib
    2 Publications Verification

    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.
  • HY-151533
    PBRM1-BD2-IN-6

    		Epigenetic Reader Domain 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.
  • HY-154984
    JET-209

    		PROTACs Histone Acetyltransferase Cancer
    JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 contains Lenalidomide (HY-A0003) (the cereblon ligand), a linker and GNE-207 (HY-120028) (bromodomain Inhibitor). JET-209 is used for cancer research.
  • HY-151534
    PBRM1-BD2-IN-7

    		Epigenetic Reader Domain Cancer
    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.
  • HY-112610
    CF53

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    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.
  • HY-114204
    GSK8814

    		Epigenetic Reader Domain Cancer
    GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.
  • HY-128341
    ERK5-IN-2

    		ERK Cancer Cardiovascular Disease
    ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
  • HY-110374
    NVS-CECR2-1

    		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.
  • HY-151528
    PBRM1-BD2-IN-1

    		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.
  • HY-151529
    PBRM1-BD2-IN-2

    		Epigenetic Reader Domain Cancer
    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.
  • HY-143332
    TRIM24/BRPF1-IN-2

    		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.
  • HY-150797
    QA-68

    QA-68-ZU81

    		 Epigenetic Reader Domain Cancer Inflammation/Immunology
    QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines. QA-68 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-151531
    PBRM1-BD2-IN-4

    		Epigenetic Reader Domain 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.
  • HY-151538
    PBRM1-BD2-IN-8

    		Epigenetic Reader Domain Cancer
    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.
  • HY-150684
    GXH-II-052

    		Epigenetic Reader Domain Cancer
    GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc.
  • 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.
  • HY-150683
    NC-III-49-1

    		Epigenetic Reader Domain Cancer
    NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc.
  • 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).
  • HY-145260
    BRD4/CK2-IN-1

    		Epigenetic Reader Domain Casein Kinase Apoptosis Autophagy Cancer
    BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
  • HY-129937A
    GNE-987

    		PROTACs Epigenetic Reader Domain Cancer
    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).
  • HY-151364
    HDAC6/8/BRPF1-IN-1

    		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.
  • HY-151532
    PBRM1-BD2-IN-5

    		Epigenetic Reader Domain Cancer
    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.