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-144236
    ZLD2218
    		99.24%
    Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis ，and ZLD2218 exhibited the most potent inhibitory activity against BRD4, with the IC50 value of 107 nM
    ZLD2218
  • HY-153226
    BET-IN-14
    		Inhibitor 98.87%
    BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 has anti-cancer activity.
    BET-IN-14
  • HY-18372
    UNC1021
    		Inhibitor 99.85%
    UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM.
    UNC1021
  • HY-170380
    XY221
    		Inhibitor
    XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
    XY221
  • HY-126299
    NVS-BPTF-1
    		Inhibitor 99.6%
    NVS-BPTF-1, a chemical probe, is a selective inhibitor for bromodomain and PHD finger containing transcription factor (BPTF), with KD of 71 nM.
    NVS-BPTF-1
  • HY-151812
    CBP/p300-IN-20
    		Inhibitor 98.03%
    CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.
    CBP/p300-IN-20
  • HY-147046
    ET-JQ1-OH
    		Inhibitor
    ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).
    ET-JQ1-OH
  • HY-160694
    cBu-Cit-GAL-02-221
    		Degrader
    cBu-Cit-GAL-02-221 is a PROTAC that degrades BRD4 by association with cBu-Cit. cBu-Cit-GAL-02-221 can effectively inhibit BRD4 in HER2 positive and negative breast cancer cell lines. cBu-Cit-GAL-02-221 has a single bond and can be conjugated to an ADC antibody to form a PAC.
    cBu-Cit-GAL-02-221
  • HY-156568A
    SMD-3040 TFA
    		Degrader 99.90%
    SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 TFA
  • HY-161346
    EBET-1055
    		Degrader
    EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures. Pink: BET ligand (HY-161387); Blue: CRBN ligase ligand (HY-14658); Black: linker
    EBET-1055
  • HY-107425B
    cis-MZ 1 hydrate
    		Inhibitor 99.0%
    cis-MZ 1 hydrate is a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The Kd of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively.
    cis-MZ 1 hydrate
  • HY-169355
    TrimTAC1
    		Degrader
    TrimTAC1 is a TRIM21-based PROTAC targeting BRD4. TrimTAC1 selectively degrads NUP98FG-mEGFP-BRD4BD2 nuclear condensates. TrimTAC1 does not degrade soluble mEGFP-BRD4BD2 in A549 cells. (Pink: target protein ligand (+)-JQ-1 (HY-13030); Blue:E3 ligase ligand Acepromazine-OTs (HY-169356); Black: PROTAC linker (HY-W088456); E3 ligase ligand + linker: HY-169357).
    TrimTAC1
  • HY-176521A
    AR/BRD4 RIPTAC-1 TFA
    		Inhibitor 99.61%
    AR/BRD4 RIPTAC-1 (Compound II-5) TFA is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 TFA induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 TFA inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 TFA holds promise for use in prostate cancer research.
    AR/BRD4 RIPTAC-1 TFA
  • HY-162739
    SMARCA2-IN-1
    		Inhibitor 98.57%
    SMARCA2-IN-1 (Compound I-19) is an inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 with IC50 >1000 nM in H1299.
    SMARCA2-IN-1
  • HY-161651
    BRD4 ligand 6
    BRD4 ligand 6 is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650).
    BRD4 ligand 6
  • HY-169094
    PFI-6-COOH
    PFI-6-COOH (Compound 18) is an eleven-nineteen leukemia (ENL) ligand, and can be used for synthesis of MS41 (HY-169093), an ENL PROTAC degrader.
    PFI-6-COOH
  • HY-N6901
    Luteolin 7-sulfate
    Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
    Luteolin 7-sulfate
  • HY-147202
    BRD4 Inhibitor-24
    		Inhibitor 99.27%
    BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A).
    BRD4 Inhibitor-24
  • HY-147868
    DC-CPin711
    		Inhibitor 99.09%
    DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis.
    DC-CPin711
  • HY-176071
    TEC 4
    		Degrader
    TEC 4 is a ByeTAC (Bypassing E-Ligase-Targeting Chimera) BRD4 degrader, with 33% BRD4 remaining at 500 nM in Ramos B-cells. TEC 4 shows toxicity for Ramos B-cells, with an IC50 of 30.5 nM. ByeTACs directly recruits a protein to the proteasome via interactions with Rpn-13 for degradation. Pink: BRD4 lignad (HY-78695); Blue: Rpn-13 ligand (HY-159808); Black: linker (HY-W008352).
    TEC 4
Cat. No. Product Name / Synonyms Application Reactivity