2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain

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Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.

The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.

p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18665
    GSK-5959
    		Inhibitor 98.74%
    GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.
    GSK-5959
  • HY-19810
    MI-538
    		Inhibitor 98.67%
    MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
    MI-538
  • HY-112609
    QCA570
    		Inhibitor 99.95%
    QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC50 of 10 nM for BRD4 BD1 Protein.
    QCA570
  • HY-111485
    INCB-057643
    		Inhibitor 98.29%
    INCB-057643 is a novel, orally bioavailable BET inhibitor.
    INCB-057643
  • HY-112804
    SGC-iMLLT
    		Inhibitor 99.33%
    SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively.
    SGC-iMLLT
  • HY-103632
    PROTAC BRD9 Degrader-1
    		Inhibitor 99.16%
    PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
    PROTAC BRD9 Degrader-1
  • HY-156828
    MMH2
    		Degrader 98.03%
    MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2).
    MMH2
  • HY-108350
    MI-2-2
    		Inhibitor 99.92%
    MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation.
    MI-2-2
  • HY-109050
    Alobresib
    		Inhibitor 98.04%
    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.
    Alobresib
  • HY-151538
    PBRM1-BD2-IN-8
    		Inhibitor 99.48%
    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.
    PBRM1-BD2-IN-8
  • HY-110218
    CW 008
    		Agonist 98.15%
    CW 008, a derivative of pyrazole-pyridine, is a CREB or PKA pathway agonist. CW 008 also is a stem cell differentiating agent. CW 008 stimulates osteoblast differentiation of human MSCs and increases bone formation in ovariectomized mice. CW008 promotes osteogenesis by activating cAMP/PKA/CREB signaling pathway and inhibiting leptin secretion.
    CW 008
  • HY-112316
    BAY1238097
    		Inhibitor 99.02%
    BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
    BAY1238097
  • HY-144897
    FHT-1204
    		Inhibitor 99.81%
    FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70).
    FHT-1204
  • HY-138563
    GSK973
    		Inhibitor 99.97%
    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-123621
    GNE-375
    		Inhibitor 99.93%
    GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin.
    GNE-375
  • HY-132889
    BPTF-IN-BZ1
    		Inhibitor 98.31%
    BPTF-IN-BZ1, a BPTF inhibitor, possesses a high potency (Kd = 6.3 nM).
    BPTF-IN-BZ1
  • HY-112504
    INCB054329
    		Inhibitor 98.00%
    INCB054329 is a potent BET inhibitor.
    INCB054329
  • HY-126428
    ZL0580
    		Modulator 99.26%
    ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.
    ZL0580
  • HY-125232
    MS645
    		≥98.0%
    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-125837A
    MS31 trihydrochloride
    		Inhibitor ≥98.0%
    MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
    MS31 trihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity