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-145946
    BRM/BRG1 ATP Inhibitor-2
    		Inhibitor 99.67%
    BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the research of BAF-related disorders.
    BRM/BRG1 ATP Inhibitor-2
  • 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-160528
    IBG3
    		Inhibitor 98.53%
    IBG3 is a dual-JQ1-containing BET molecular glue degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively.
    IBG3
  • HY-13959
    MS436
    		Inhibitor 99.94%
    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.
    MS436
  • HY-156214
    NICE-01
    		99.53%
    NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins.
    NICE-01
  • 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
  • HY-19553
    LP99
    		Inhibitor 99.18%
    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-169093
    MS41
    		Degrader
    MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078).
    MS41
  • HY-156568B
    SMD-3040 formate
    		Degrader 99.78%
    SMD-3040 formate is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 formate can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 formate can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 formate
  • HY-149420
    BRD7-IN-2
    		Inhibitor 99.21%
    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.
    BRD7-IN-2
  • 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-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-159989
    UNC10142
    		Antagonist 99.74%
    UNC10142 (Compound 44) is a first-in-class small molecule antagonist of CHD1 that binds with an IC50 value of 1.7 μM. UNC10142 leads to a dose-dependent reduction in viability in PTEN-deficient prostate cancer cells.
    UNC10142
  • HY-101027A
    GSK4028
    		98.06%
    GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK4028
  • HY-126428
    ZL0580
    		Modulator 99.42%
    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-145310
    ZL0590
    		Inhibitor 99.86%
    ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities. ZL0590 can reduce mucosal inflammation in animal models of inflammatory bowel disease and restores tissue architecture. ZL0590 can be used in research on inflammatory diseases such as inflammatory bowel disease.
    ZL0590
  • HY-13032B
    Molibresib besylate
    		Inhibitor
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
    Molibresib besylate
  • HY-156827
    MMH1
    		Degrader 98.08%
    MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2).
    MMH1
  • HY-157486
    KMI169
    		Inhibitor 98.00%
    KMI169 is a potent and selective inhibitor targeting lysine methyl-transferase (KMT9) (IC50 = 0.05 μM, Kd = 0.025 μM). KMI169 functions as a bi-substrate inhibitor targeting the cofactor S-5’-adenosyl-L-methionine (SAM) and substrate binding pockets of KMT9. KMI169 can downregulate target genes involved in cell cycle regulation and impair proliferation of tumor cells by inhibiting KMT9. KMI169 is a valuable tool to probe cellular KMT9 functions and can be research for combating diseases including prostate, lung, colon, and invasive bladder cancer.
    KMI169
  • HY-151594
    iBRD4-BD1
    		Inhibitor 98.65%
    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
Cat. No. Product Name / Synonyms Application Reactivity