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Epigenetic Reader Domain

Epigenetic reader domains can be thought of as effector proteins that recognize and are recruited to specific epigenetic marks.

  • VTP50469
    T133362169916-18-9
    VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.
    • $177
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  • ARV-771
    T54351949837-12-0
    Glycodeoxycholic Acid is an endogenous metabolite, a natural product found in Streptomyces niger, Trypanosoma brucei, and Cryptomonas, which induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis.
    • $55
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    TargetMol | Inhibitor Hot
  • Curcumin
    T1516458-37-7
    Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
    • $30
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • SNDX-5613
    T129432169919-21-3
    SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias.
    • $67
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    TargetMol | Inhibitor Hot
  • (+)-JQ-1
    T21101268524-70-4
    (+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
    • $30
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    TargetMol | Citations Cited
  • 666-15
    T53181433286-70-4
    666-15 (CREB inhibitor) is a potent and selective CREB inhibitor (IC50: 81 nM).
    • $52
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • ICG-001
    T6113780757-88-2
    ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.
    • $30
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    TargetMol | Citations Cited
  • AU-15330
    T399542380274-50-8In house
    AU-15330 is a protein hydrolysis-targeted chimeric (PROTAC) degrader of the SWI/SNF ATPase subunits SMARCA2 and SMARCA4.AU-15330 potently inhibits tumor growth in a prostate cancer xenograft model and acts synergistically with the AR antagonist enzalutamide.AU-15330 shows partial therapeutic efficacy and non-toxicity with the AR antagonist enzalutamide in a desmoplasia-resistant prostate cancer (CRPC) model. AU-15330 showed partial therapeutic efficacy in a denervation-resistant prostate cancer (CRPC) model and AU-15330 was characterized by non-toxicity.
    • $139
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    TargetMol | Inhibitor Hot
  • Naphthol AS-E
    T785692-78-4
    Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.
    • $33
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  • Bisdemethoxycurcumin
    TL000724939-16-0
    Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].
    • $41
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  • CPI203
    T2442202591-23-9
    CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
    • $50
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  • OXF BD 02
    T231151429129-68-9
    OXF BD 02 is a potent and selective BRD4(1) inhibitor (IC50: 382 nM) with anticancer and anti-inflammatory activity.
    • $100
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  • 6-Bromo-3-methyl-1,4-dihydroquinazolin-2-one
    T8609328956-24-7
    CHEMBRDG-BB 7118966 is an inhibitor of Bromodomain-containing protein 4 (human).
    • $133
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  • Pocenbrodib
    T696912304372-79-8In house
    Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.
    • $790
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  • PBRM1-BD2-IN-3
    T601582819989-58-5In house
    PBRM1-BD2-IN-3 (compound 12) is a potent inhibitor of PBRM1-BD2, exhibiting an IC50 value of 1.1 μM, and is utilized in anticancer research.
    • $117
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  • UNC926 hydrochloride
    T92211782573-49-2
    UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor.
    • $133
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  • PBRM1-BD2-IN-7
    T601552819989-68-7In house
    PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.
    • $117
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  • PNZ5
    T125131629277-36-6In house
    PNZ5, an isoxazole-based pan-BET inhibitor, demonstrates potent activity and high selectivity comparable to the established (+)-JQ1, exhibiting a dissociation constant (KD) of 5.43 nM for BRD4(1).
    • $195
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  • SMARCA-BD ligand 1 for Protac
    T138481997319-92-2In house
    SMARCA-BD ligand 1 for Protac is a compound capable of binding to SMARCA2, the BAF ATPase subunit, based on the Protac technology for degrading SMARCA2
    • $197
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  • ICG001
    T2237847591-62-2
    ICG001 (PRI-724 isomer) antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.
    • $30
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    TargetMol | Citations Cited
  • 1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one
    T8601218934-50-0
    1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one is an inhibitor Bromodomain-containing protein 4 (human).
    • $133
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  • 2-methyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-4-one
    T5001496680-77-2
    2-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one is ligand of CBP.
    • $50
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  • CDD-1102 HCl
    T72058L In house
    CDD-1102 HCl is a novel BRDT-BD4 / BRD2-BD1302 selective inhibitor that shows non-hormonal contraceptive potential in ex vivo experiments.
    • $350
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  • ZEN-3411
    T133931952264-36-6In house
    ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.
    • $350
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  • PBRM1-BD2-IN-2
    T601562819989-57-4In house
    PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.
    • $117
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  • GSK778 hydrochloride
    T9703L2863657-79-6
    GSK778 hydrochloride hydrochloride 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 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].
    • $117
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  • BRD4 Inhibitor-27
    T78555930039-92-2
    BRD4 Inhibitor-27 is a potent BRD4 inhibitor that inhibits BRD4 BD1 and BRD4 BD2 with IC50s of 9.6 and 11.3 μM, respectively.BRD4 Inhibitor-27 has anticancer activity and can be used for breast cancer research.
    • $195
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  • CCT077791
    T25215748777-47-1In house
    CCT077791 is a potent inhibitor of p300 and PCAF histone acetyltransferase activity for cancer research.
    • $1,520
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  • Piflufolastat
    T312241423758-00-2In house
    Piflufolastat (DCFPYL) is a PET imaging agent for prostate cancer PSMA. It is a fluorinated prostate-specific membrane antigen (PSMA) preparation. Piflufolastat can be used to prepare piflufolastat F 18 (DCFPyL F-18).
    • $258
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  • CPI-0610 carboxylic acid
    T108791380089-81-5In house
    CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.
    • $526
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  • BY27
    T106382247236-59-3In house
    BY27 is a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1/BD2 of BRD2, BRD3, BRD4 and BRDT, and suppresses tumor growth.
    • $483
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  • AW68
    T10638L2247236-61-7In house
    AW68 is a potential small molecule BRD4 inhibitor that prevents and treats BRD4-related diseases and can be used in cancer research.
    • $195
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  • 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one
    T5000624365-65-9
    3-methyl-1,2,3,4-tetrahydroquinazolin-2-one is a inhibitor of BRD4 .
    • $50
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  • FT001
    T273921778655-51-8In house
    FT001 is a potent, selective and orally available inhibitor of BET Bromodomain with antitumor activity. FT001 inhibited the expression of MYC with the IC50 value of 0.46 μM). FT001 has potent antiproliferative effects against MV-4-11 and demonstrates significant MYC mRNA suppression both in vitro and in vivo.
    • $117
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  • 3-methyl-1,2-dihydroquinolin-2-one
    T500352721-59-7
    3-methyl-1,2-dihydroquinolin-2-one is the first known micromolar inhibitors of the ATAD2 bromodomain.
    • $76
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  • BRD4-BD1-IN-2
    T641172761321-26-8
    BRD4-BD1-IN-2 is a selective and potent BRD4-BD1 inhibitor with an IC50 value of 2.51 µM, which is 20-fold greater than the inhibitory activity against BRD4-BD2.BRD4-BD1-IN-2 can be used in the study of cardiovascular and cancer-related diseases.
    • $397
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  • MS31 trihydrochloride (2366264-12-0 free base)
    T12111L
    MS31 trihydrochloride (2366264-12-0 free base) is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor.
    • $205
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  • GNE-049
    T153971936421-41-8In house
    GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
    • $523
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  • NHWD-870
    T365732115742-03-3In house
    NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.
    • $1,630
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  • BETd-260
    T145502093388-62-4In house
    BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.
    • $212
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  • FKBP12 PROTAC dTAG-7
    T112922064175-32-0In house
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.
    • $1,280
    35 days
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  • Crebinostat
    T270831092061-61-4In house
    Crebinostat is a potent histone deacetylase (HDAC) inhibitor, inhibiting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively.Crebinostat increases the density of synapsin-1 punctae along dendrites in neurons in vitro. Crebinostat increased the density of synapsin-1 punctae along dendrites in neurons in vitro. crebinostat modulated chromatin-mediated neuroplasticity and enhanced memory in mice. crebinostat induced histone H3 and histone H4 acetylation and enhanced the expression of the cAMP-responsive element binding protein (CREB) target gene, Egr1. Crebinostat induces histone H3 and histone H4 acetylation and enhances the expression of Egr1, a cAMP response element binding protein (CREB) target.
    • $350
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  • OXFBD04
    T123382231747-03-6In house
    OXFBD04 is a potent and selective BRD4 inhibitor (IC50= 166 nM). OXFBD04 is a potent BET bromodomain ligand and exhibits additional modest affinity for the CREBBP bromodomain. OXFBD04 exhibits anti-cancer activity.
    • $97
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  • TCIP 1
    T79801 In house
    TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].
    • $2,420
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  • ABBV-744
    T46972138861-99-9In house
    ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.
    • $39
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  • NEO2734
    T86582081072-29-7In house
    NEO2734 (EP31670) is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).
    • $116
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  • CF53
    T107731808160-52-2In house
    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.
    • $88
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  • CeMMEC1
    T4345440662-09-9In house
    CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).
    • $30
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  • LT052
    T118872543545-44-2In house
    LT052, a highly active and selective BET BD1 inhibitor with an IC50 of 87.7 nM, demonstrates nanomolar BRD4 BD1 potency and significant selectivity, being 138-fold more selective for BRD4 BD1 over BRD4 BD2 (IC50 =12.130 μM). Its anti-inflammatory properties make it a potential candidate for acute gout arthritis research [1].
    • $1,490
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  • PBRM1-BD2-IN-8
    T601572819989-75-6In house
    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.
    • $98
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