2. Epigenetics
  3. Epigenetic Reader Domain

Epigenetic Reader Domain

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.

Epigenetic Reader Domain Related Products (694):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 Inhibitor 99.90%
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2].
  • HY-134653
    5-Ph-IAA Inhibitor
    5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression[1].
  • HY-13823
    C646 Inhibitor 99.88%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases[1].
  • HY-107455
    A-485 Inhibitor
    A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively[1].
  • HY-N0005
    Curcumin Inhibitor 98.84%
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • HY-172827
    PROTAC BRD4 Degrader-30 Degrader
    PROTAC BRD4 degrader-30 is an ISOX-DUAL-Based PROTAC degrader selectively targeting BRD4 (IC50 = 65 nM). PROTAC BRD4 degrader-30 can be used for research of c-Myc oncoprotein and cancer cell pathophysiology. (Pink: BRD4 ligand (HY-172828); Blue: CRBN ligand (HY-103596); Black: linker (HY-Y0139); CRBN ligand+linker: HY-138847)[1].
  • 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); Rpn-13 ligand (HY-159808); linker: HY-W008352[1].
  • HY-176056
    Hedgehog IN-9 Agonist
    Hedgehog IN-9 (compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe[1].
  • HY-133136
    PROTAC BRD4 Degrader-2 Inhibitor
    PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1[1].
  • HY-173351
    G-6599 Degrader
    G-6599 is a SMARCA2/A4 target-anchored monovalent degrader with DC50 values of 0.018 nM and 0.056 nM, respectively. G-6599 has degradation activity and anti-proliferative effects in AR-dependent prostate cancer cell lines[1].
  • HY-133131
    PROTAC BRD4 Degrader-1 Inhibitor 99.12%
    PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression[1].
  • HY-149761
    GSK023 Chemical
    GSK023 (compound 31) is a selective chemical probe targeting the BET BD1 domain[1].
  • 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)[1].
  • HY-153242
    GSK217 Inhibitor
    GSK217 is a potent, selective, and highly soluble bromo and extraterminal domain (BET) second bromodomain (BD2) inhibitor. GSK217 can be used for the research of oncology and immune inflammation research[1].
  • HY-15826
    SGC-CBP30 Inhibitor 99.83%
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects[1][2][3].
  • HY-139861
    CBP/p300-IN-14 Inhibitor
    CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC50 of 3.3 nM (extracted from patent WO2021213521A1, compound 27)[1].
  • HY-138555
    PROTAC BRD4 Degrader-8 Inhibitor 99.45%
    PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].
  • HY-169994
    BC13 Inhibitor
    BC13 is a CDK6/BRD4 inhibitor with the IC50 values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels[1].
  • HY-142954
    UNC6212 (Kme2) Inhibitor
    UNC6212 (Kme2), a dimethyllysine (Kme2)-containing ligand, has a KD for CBX5 of 5.7 μM[1].
  • HY-163811
    BRD9 Degrader-4 Inhibitor
    BRD9 Degrader-4 (BRD9c), a bifunctional molecular glue, is a potent BRD9 degrader with a DC50 of ≤25 nM. BRD9 Degrader-4 has anti-cancer effects[1].