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-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-101146
    SF2523
    		Inhibitor 99.34%
    SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
    SF2523
  • HY-13960
    GSK1324726A
    		Inhibitor 99.92%
    GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
    GSK1324726A
  • HY-12518
    OF-1
    		Inhibitor 98.93%
    OF-1, a chemical probe, is a potent pan-BRPF bromodomain (BRD) inhibitor, with IC50 values of 270 nM, 1.2 μM for TRIM24 and BRPF1B, respectively.
    OF-1
  • 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-153459
    IBG1
    		Degrader 99.88%
    IBG1 is a molecular glue degrader targeting BRD2 and BRD4 (DC50: 0.15 nM). IBG1 has no significant degradation effect on its paralogue BRD3. IBG1 can inhibit the growth of cancer cells and can be used in tumor research. (Pink: BRD2/BRD4 Ligand (HY-111139); Black: Linker; Blue: DCAF15 ligand-1 (HY-W037495)).
    IBG1
  • HY-151532
    PBRM1-BD2-IN-5
    		Inhibitor 99.75%
    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.
    PBRM1-BD2-IN-5
  • 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-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-101519
    BETd-260
    		Inhibitor 99.68%
    BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
    BETd-260
  • 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-133736
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
    		99.73%
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader (MZ 1 (HY-107425) analog) and PEG-based linker. PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can be used for the research of HER2-positive breast cancer.
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
  • HY-114162A
    VTP50469 fumarate
    		Inhibitor 99.79%
    VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.
    VTP50469 fumarate
  • 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-111976
    MT1
    		Inhibitor 99.69%
    MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1).
    MT1
  • HY-156828
    MMH2
    		Degrader 98.95%
    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-18665
    GSK-5959
    		Inhibitor 99.73%
    GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.
    GSK-5959
  • 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-156744
    DBr-1
    		Degrader 98.87%
    DBr-1 is a potent BRD9 PROTAC degrader (KD: 13 nM). DBr-1 can overcome intrinsic resistance to VHL-degrader. Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BRD9/BRD7 bromodomains inhibitor (HY-100352).
    DBr-1
Cat. No. Product Name / Synonyms Application Reactivity