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-139294
    PROTAC BRD4 Degrader-15
    		Inhibitor
    PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-15
  • HY-168248
    BRM/BRG1 ligand 2
    BRM/BRG1 ligand 2 is the ligand for target protein, which can be used for synthesis of PROTAC BRM/BRG1 degrader-2 (HY-168247).
    BRM/BRG1 ligand 2
  • HY-142705
    BRD4 D1-IN-2
    		Inhibitor
    BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.
    BRD4 D1-IN-2
  • HY-172124
    PROTAC BRD4 Degrader-29
    		Degrader
    PROTAC BRD4 Degrader-29 (compound 7a) is a potent PROTACs degrader of BRD4, with the DC50 of 89.4 nM. PROTAC BRD4 Degrader-29 plays an important role in cancer research (Pink: ligand for target protein (HY-13030); Black: linker (HY-172125); Blue: E3 ligase ligand (HY-103597)).
    PROTAC BRD4 Degrader-29
  • HY-176035
    MS479
    		Degrader
    MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038).
    MS479
  • HY-162835
    PROTAC SMARCA2/4-degrader-28
    		Degrader
    PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a PROTAC-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)).
    PROTAC SMARCA2/4-degrader-28
  • HY-163460
    MS8535
    		Inhibitor
    MS8535 is a SPIN1 selective inhibitor, with an IC50 of 0.2 μM.
    MS8535
  • HY-168242
    PROTAC BRM/BRG1 degrader-1
    		Inhibitor
    PROTAC BRM/BRG1 degrader-1 (Example 253) is a PROTAC BRM/BRG1 degrader, with DC50 of 10-100 nM for BRM, > 1 μM for BRG1. PROTAC BRM/BRG1 degrader-1 can be used for cancer research. Blue: E3 ligase ligand (HY-168243), black: linker (HY-168244). Red: BRM/BRG1 inhibitor (HY-W539427).
    PROTAC BRM/BRG1 degrader-1
  • HY-156774
    CCW 28-3
    		Degrader
    CCW 28-3 is a PROTAC-based BRD4 degrader in a proteasome- and RNF4-dependent manner (Pink: JQ-1 (carboxylic acid) (HY-78695); Black: linker (HY-170384); Blue: RNF4 ligand CCW16 (HY-143346)).
    CCW 28-3
  • HY-129937
    (S)-GNE-987
    		Inhibitor
    (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
    (S)-GNE-987
  • HY-P10446
    TAT-PiET-PROTAC
    		Inhibitor
    TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.
    TAT-PiET-PROTAC
  • HY-169170
    PARP1/BRD4-IN-3
    		Inhibitor
    PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy.
    PARP1/BRD4-IN-3
  • HY-160662
    BRD4-IN-5
    		Inhibitor
    BRD4-IN-5 (example 51) is a BRD4 inhibitor. The Ki values of the two BRD4 domains BDI_K57-E168 and BDII_E352-M457 are 9.7 nM and 16.1 nM, respectively. BRD4-IN-5 can be used in cancer research.
    BRD4-IN-5
  • HY-136192
    TP-472N
    TP-472N is a negative control probe for TP-472. TP-472 is a potent and selective BRD7/9 probe.
    TP-472N
  • HY-177141
    CDD-1154
    		Inhibitor
    CDD-1154 is an aminopyrimidine analog. CDD-1154 is a BRDT-BD2 inhibitor (IC50: 139 nM). CDD-1154 is used in male contraceptive research.
    CDD-1154
  • HY-157460
    BRD4 Inhibitor-29
    BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells.
    BRD4 Inhibitor-29
  • HY-156401
    BRD9 Degrader-1
    		Inhibitor
    BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader. BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062). (Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695).
    BRD9 Degrader-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); Blue: Rpn-13 ligand (HY-159808); Black: linker (HY-W008352).
    TEC 4
  • HY-169151
    PROTAC BRD4-DCAF1 degrader-1
    PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)).
    PROTAC BRD4-DCAF1 degrader-1
  • HY-163152
    PROTAC BRM degrader-1
    		Inhibitor
    PROTAC BRM degrader-1 (compound 17) is a PROTAC-based BRM and BRG1 degrader, with DC50 values of 93 pM and 4.9 nM, respectively.
    PROTAC BRM degrader-1
Cat. No. Product Name / Synonyms Application Reactivity