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-172130
    PI3Kδ/BET-IN-1
    		Inhibitor
    PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC50 = 112 nM) and BRD4-BD1 (IC50 = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells.
    PI3Kδ/BET-IN-1
  • HY-176535
    KB-0118
    		Inhibitor
    KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
    KB-0118
  • HY-146741
    SDR-04
    		Inhibitor
    SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.
    SDR-04
  • HY-170347
    PROTAC SMARCA2/4 degrader-36
    		Degrader
    PROTAC SMARCA2/4 degrader-36 (Compound 29) is an effective dual degrader of SMARCA2/4,with DC50 values of 0.22 nM and 0.85 nM for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2/4 degrader-36 has anti-cell proliferation activity (Pink: Target Protein Ligand (HY-170354); Black: Linker (HY-W895794); Blue: E3 Ligase Ligand (HY-170353); E3 Ligase Ligand-Linker Conjugate (HY-170356)).
    PROTAC SMARCA2/4 degrader-36
  • HY-176476
    BRD4/FKBP12 degrader-1
    		Degrader
    BRD4/FKBP12 degrader-1(a1d) is a BRD4/FKBP12 degrader with anti-cancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176501, linker: HY-140212).
    BRD4/FKBP12 degrader-1
  • HY-128761
    CBP/p300-IN-2
    		Inhibitor
    CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM and 5.96 nM for CBP/HTRF and Myc, respectively. CBP/EP300-IN-2, example 25, is extracted from patent WO2017205538A1.
    CBP/p300-IN-2
  • HY-144338
    PARP1/BRD4-IN-1
    		Inhibitor
    PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.
    PARP1/BRD4-IN-1
  • HY-178488
    BRM/BRG1 ATP-IN-7
    		Inhibitor
    BRM/BRG1 ATP-IN-7 (Compound Cpd69) is a selective dual BRM (SMARCA2) and BRG1 (SMARCA4) inhibitor with IC50 values of 12 nM and 8 nM, respectively. BRM/BRG1 ATP-IN-7 is promising for research of BRM/BRG1-dependent cancers (e.g., non-small cell lung cancer, Ewing sarcoma) and virus-associated diseases (e.g., HPV infection).
    BRM/BRG1 ATP-IN-7
  • HY-150683
    NC-III-49-1
    		Inhibitor
    NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc.
    NC-III-49-1
  • HY-173315
    pan-BET/BD2-IN-1
    		Inhibitor
    pan-BET/BD2-IN-1 (compound 6b) is a selective extra-terminal (BET) protein inhibitor (BRDT-1 Ki = 1.05 μM and BRD4-1 Ki = 0.68 μM). pan-BET/BD2-IN-1 inhibits MM.1S cancer cell growth with an IC50 of 2.6 μM.
    pan-BET/BD2-IN-1
  • HY-151530
    PBRM1-BD2-IN-3
    		Inhibitor
    PBRM1-BD2-IN-3 (compound 12) is a potent PBRM1-BD2 inhibitor with an IC50 value of 1.1 μM. PBRM1-BD2 Inhibitor can be used to research anticancer.
    PBRM1-BD2-IN-3
  • HY-170824
    SMD-3236
    		Degrader
    SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827).
    SMD-3236
  • HY-177144
    CDD-1128
    		Inhibitor
    CDD-1128 (Compound 11) is a potent inhibitor of BRDT-BD2. CDD-1128 has an IC50 of 521 nM against BRDT-BD2. CDD-1128 can be studied in research on nonhormonal contraceptive agent.
    CDD-1128
  • HY-163870
    PROTAC SMARCA2/4-degrader-17
    		Degrader
    PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W053507); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-17
  • HY-111979
    ZEN-3411
    		Inhibitor
    ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4.
    ZEN-3411
  • HY-50698G
    BI 2536 (GMP)
    		Inhibitor
    BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.
    BI 2536 (GMP)
  • HY-169980
    Mivebresib-alkyne
    		Control
    Mivebresib-alkyne (Compound 25), a Mivebresib (HY-100015) derivative, can be used for BRD4 targeted PROTAC synthesis through click reaction.
    Mivebresib-alkyne
  • HY-162813
    PROTAC SMARCA2/4-degrader-25
    PROTAC SMARCA2/4-degrader-25 (compound 7d) is a PROTAC targeting SMARCA2/4. PROTAC SMARCA2/4-degrader-25 is composed of E3 ligase (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and target protein ligand SMARCA2/4-ligand-3 (HY-162814) (red part). The conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845)[1].
    PROTAC SMARCA2/4-degrader-25
  • HY-178225
    PROTAC SMARCA2/4 degrader-39
    		Degrader
    PROTAC SMARCA2/4 degrader-39 (Compound 7) is a selective degrader of SMARCA2 (BRM) and SMARCA4 (BRG1) PROTAC. PROTAC SMARCA2/4 degrader-39 is promising for research of oncology, such as non-small cell lung cancer and colorectal cancer. (Pink: BRM/BRG1 ligand 5 (HY-178886); Black: Linker Piperazine (HY-B0912); Blue: (S)-Deoxy-thalidomide (HY-168055))
    PROTAC SMARCA2/4 degrader-39
  • HY-168634
    SJ46421
    		Inhibitor
    SJ46421 is a (+)-JQ-1 (HY-13030) based KLHDC2-BRD3 PROTAC protein degrader. SJ46421 induces cooperative ternary complexes with KLHDC2 and BRD3BD2, with an IC50 of 7.8 nM. SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation. SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4. SJ46421 possesses poor cell permeability. (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-168536)).
    SJ46421
Cat. No. Product Name / Synonyms Application Reactivity