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-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-181758
    PROTAC CBP/p300/BRD4 Degrader-1
    		Degrader
    PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer.
    PROTAC CBP/p300/BRD4 Degrader-1
  • 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-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
  • HY-P10445
    TAT-PiET
    		Inhibitor
    TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET can be used for the research of cancer, such as breast cancer.
    TAT-PiET
  • HY-143235
    BRD4 Inhibitor-15
    		Inhibitor
    BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research.
    BRD4 Inhibitor-15
  • HY-149863
    DDO-8926
    		Inhibitor
    DDO-8926 is a potent and selective BET inhibitor that can significantly reduce mechanical hypersensitivity by inhibiting the expression of pro-inflammatory cytokines and reducing excitability for neuropathic pain research.
    DDO-8926
  • HY-163019
    EN884
    		Degrader
    EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs).
    EN884
  • HY-162743
    PROTAC SMARCA2/4-degrader-29
    		Degrader
    PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-29 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-29
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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