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-160528
    IBG3
    		Inhibitor 98.53%
    IBG3 is a Molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia.
    IBG3
  • HY-138563
    GSK973
    		Inhibitor 99.97%
    GSK973, a chemical probe, 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-19810
    MI-538
    		Inhibitor 98.23%
    MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
    MI-538
  • 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-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-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-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-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-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-130622
    LT052
    		Inhibitor 98.02%
    LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research.
    LT052
  • HY-112150
    ZL0454
    		Inhibitor
    ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
    ZL0454
  • HY-148116
    DN02
    		Inhibitor 98.68%
    DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8 (1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki>1000 nM).
    DN02
Cat. No. Product Name / Synonyms Application Reactivity