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-168182
    Menin-MLL inhibitor 34
    		Inhibitor
    Menin-MLL inhibitor 34 (Compound 37) is a selective and potent Menin-MLL inhibitor, with an IC50 of 18.21 nM for Menin. Menin-MLL inhibitor 34 has long-lasting anti-leukemic effects by reducing Menin protein levels and down-regulating MEN1 transcription.
    Menin-MLL inhibitor 34
  • HY-161769
    HL435
    		Inhibitor
    HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
    HL435
  • HY-178984
    PI3Kα-IN-28
    		Inhibitor
    PI3Kα-IN-28 is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 (IC50 = 1.46 µM) and KYSE450 (IC50 = 0.57 µM) cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer.
    PI3Kα-IN-28
  • HY-163798
    Menin-MLL inhibitor 33
    		Inhibitor
    Menin-MLL inhibitor 33 (compound 15-a) is a potent Menin-MLL inhibitor with an IC50 value of 3.6 nM. Menin-MLL inhibitor 33 shows antiproliferative activity.
    Menin-MLL inhibitor 33
  • HY-153820
    PROTAC BRD4 Degrader-20
    		Degrader
    PROTAC BRD4 Degrader-20 (compound 195) is an bifunctional compound and an degrader of BRD4.
    PROTAC BRD4 Degrader-20
  • HY-149948
    PROTAC BRD3/BRD4-L degrader-2
    		Degrader
    PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer.
    PROTAC BRD3/BRD4-L degrader-2
  • HY-155680
    BET BD2-IN-1
    		Inhibitor
    BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research.
    BET BD2-IN-1
  • HY-169278
    PROTAC SMARCA2 degrader-26
    		Degrader
    PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity.
    PROTAC SMARCA2 degrader-26
  • HY-172210
    DDO-8958
    DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity.
    DDO-8958
  • HY-157134
    Y08262
    		Inhibitor
    Y08262 is a potent and selective CBP bromodomain inhibitor. Y08262 selectively inhibits the CBP bromodomain with an IC50 value of 73.1 nM. Y08262 can be used for the research of acute myeloid leukemia (AML).
    Y08262
  • HY-157290
    HL403
    		Inhibitor
    HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity.
    HL403
  • HY-162740
    SMARCA2-IN-2
    		Inhibitor
    SMARCA2-IN-2 (Compound I-25) is a SMARCA2 inhibitor (IC50: 101-500 μM), and can be used for cancer research.
    SMARCA2-IN-2
  • HY-162744
    PROTAC SMARCA2/4-degrader-31
    		Degrader
    PROTAC SMARCA2/4-degrader-31 (Compound I-280) is a degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-31 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-163926); Black: Linker (HY-159682); Blue: Ligand for E3 ligase (HY-W382038)).
    PROTAC SMARCA2/4-degrader-31
  • HY-175033
    BRD4-IN-11
    		Inhibitor
    BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis.
    BRD4-IN-11
  • HY-169148
    YT117R
    		Degrader
    YT117R is a PROTAC degrader of FKBP12 and Pink: Target protein ligand: (HY-158301); Black: linker (HY-42776); Blue: E3 ligase ligand (HY-78695)).
    YT117R
  • HY-167871
    BRD4 Inhibitor-36
    		Inhibitor
    BRD4 Inhibitor-36 (Compound 185) is a BRD4 inhibitor. BRD4 Inhibitor-36 can be used for the research of cancer.
    BRD4 Inhibitor-36
  • HY-168936
    DP-15
    		Degrader
    DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
    DP-15
  • HY-150268
    Zavabresib
    		Inhibitor
    Zavabresib (BET-IN-16) (Compound I) is a BET inhibitor. BET-IN-16 shows anticancer activity. Zavabresib inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively.
    Zavabresib
  • HY-174348
    BRD4-IN-10
    		Inhibitor
    BRD4-IN-10 (Compound 31) is a selective BRD4 inhibitor with an IC50 of 13.5 nM. BRD4-IN-10 can exert anti-inflammatory and anti-fibrotic effects. BRD4-IN-10 also has good metabolic stability, pharmacokinetic properties and safety. BRD4-IN-10 can be used in the research of renal fibrosis diseases.
    BRD4-IN-10
  • HY-115926
    BRD4 Inhibitor-16
    		Inhibitor
    BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information.
    BRD4 Inhibitor-16
Cat. No. Product Name / Synonyms Application Reactivity