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-103633R
    PROTAC BET Degrader-1 (Standard)
    		Inhibitor
    PROTAC BET Degrader-1 (Standard) is the analytical standard of PROTAC BET Degrader-1 (HY-103633). This product is intended for research and analytical applications. PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1 (Standard)
  • HY-103299R
    KG-501 (Standard)
    		Inhibitor
    KG-501 (Standard) is the analytical standard of KG-501 (HY-103299). This product is intended for research and analytical applications. KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
    KG-501 (Standard)
  • HY-100726R
    GNE-272 (Standard)
    		Inhibitor
    GNE-272 (Standard) is the analytical standard of GNE-272 (HY-100726). This product is intended for research and analytical applications. GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
    GNE-272 (Standard)
  • HY-124284R
    Hexamethylene bisacetamide (Standard)
    		Inhibitor
    Hexamethylene bisacetamide (Standard) is the analytical standard of Hexamethylene bisacetamide. This product is intended for research and analytical applications. Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.
    Hexamethylene bisacetamide (Standard)
  • HY-170219
    RMM23
    		Inhibitor
    RMM23 is an inhibitor targeting PfBDP1 with a Kd value of 1.24 μM. RMM23 against the wild-type strains 3D7 and NF54, and the multidrug-resistant K1 strain in vitro blood stage, with EC50 values of 18 μM, 14 μM, 20 μM, respectively .
    RMM23
  • HY-78695A
    (R)-JQ-1 carboxylic acid
    		Inhibitor
    (R)-JQ-1 carboxylic acid, is an isomer of JQ-1 carboxylic acid (HY-78695). JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
    (R)-JQ-1 carboxylic acid
  • HY-109050R
    Alobresib (Standard)
    		Inhibitor
    Alobresib (Standard) is the analytical standard of Alobresib (HY-109050). This product is intended for research and analytical applications. Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.
    Alobresib (Standard)
  • HY-177140
    CDD-1147
    		Inhibitor
    CDD-1147 is a BRDT-BD2 inhibitor with an IC50 of 94 nM. CDD-1147 can be used in the research of non-hormonal contraceptives for men.
    CDD-1147
  • HY-100653AR
    AZD5153 6-Hydroxy-2-naphthoic acid (Standard)
    		Inhibitor
    AZD5153 (6-Hydroxy-2-naphthoic acid) (Standard) is the analytical standard of AZD5153 (6-Hydroxy-2-naphthoic acid) (HY-100653A). This product is intended for research and analytical applications. AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
    AZD5153 6-Hydroxy-2-naphthoic acid (Standard)
  • HY-108350R
    MI-2-2 (Standard)
    		Inhibitor
    MI-2-2 (Standard) is the analytical standard of MI-2-2 (HY-108350). This product is intended for research and analytical applications. MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation.
    MI-2-2 (Standard)
  • HY-122626
    BRPF1B/TRIM24-IN-1
    		Inhibitor
    BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC50 values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a KD of 222 nM and has a KD for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM.
    BRPF1B/TRIM24-IN-1
  • HY-155222
    TW9
    		Inhibitor
    TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026).
    TW9
  • HY-160260
    EP300/CBP-IN-1
    		Inhibitor
    EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC50s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells.
    EP300/CBP-IN-1
  • HY-100220R
    GSK6853 (Standard)
    		Inhibitor
    GSK6853 (Standard) is the analytical standard of GSK6853 (HY-100220). This product is intended for research and analytical applications. GSK6853, a chemical probe, is a potent and selective inhibitor of the BRPF1 bromodomain. GSK6853 shows excellent BRPF1 potency (pKd = 9.5) and greater than 1600-fold selectivity over all other bromodomains.
    GSK6853 (Standard)
  • HY-W173361
    CBP/p300-IN-24
    		Inhibitor
    CBP/p300-IN-24 is a selective CBP bromodomain inhibitor with an IC50 of 32 μM, showing selectivity over BRD4 BD-1 bromodomain. CBP/p300-IN-24 binds to the acetyl lysine binding pocket, forms hydrogen bonds with Asn1168 and a solvent-mediated hydrogen bond with Tyr1125, and forms hydrophobic interactions with Leu1120, Ile1122, and Val1174.
    CBP/p300-IN-24
  • HY-100697R
    TPOP146 (Standard)
    		Inhibitor
    TPOP146 (Standard) is the analytical standard of TPOP146 (HY-100697). This product is intended for research and analytical applications. TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
    TPOP146 (Standard)
  • HY-100517R
    TP-472 (Standard)
    		Inhibitor
    TP-472 (Standard) is the analytical standard of TP-472 (HY-100517). This product is intended for research and analytical applications. TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.
    TP-472 (Standard)
  • HY-107424R
    BAY-299 (Standard)
    		Inhibitor
    BAY-299 (Standard) is the analytical standard of BAY-299 (HY-107424). This product is intended for research and analytical applications. BAY-299, a chemical probe, is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
    BAY-299 (Standard)
  • HY-100352R
    BI-9564 (Standard)
    		Inhibitor
    BI-9564 (Standard) is the analytical standard of BI-9564 (HY-100352). This product is intended for research and analytical applications. BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family.
    BI-9564 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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