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.

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-179498
    ROCK2-IN-13
    		Activator
    ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach.
    ROCK2-IN-13
  • HY-D2978
    MR2-cy5
    MR2-cy5 is a fluorescent agent. MR2-cy5 is highly specific to CD206. MR2-cy5 can track CD206+ macrophages.
    MR2-cy5
  • HY-163810
    BRD9 Degrader-3
    		Degrader
    BRD9 Degrader-3 (compound B20) is a BRD9 molecular glue, with a DC50 of <1.25 nM.
    BRD9 Degrader-3
  • HY-134598
    653-47
    		Inhibitor
    653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM.
    653-47
  • HY-114902
    Y02224
    		Inhibitor
    Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research.
    Y02224
  • 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-182912
    PLX-4104
    PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia.
    PLX-4104
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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