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-142743
    Y08175
    		Inhibitor
    Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer.
    Y08175
  • HY-12625
    MIV-6
    		Inhibitor
    MIV-6 is a small molecule inhibitor that inhibits menin-mixed lineage leukemia (MLL) interaction and exhibits strong selective activity in MLL leukemia cells with IC50 = 56 nM.
    MIV-6
  • HY-146709
    BET bromodomain inhibitor 2
    		Inhibitor
    BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC50 of 14.1 µM.
    BET bromodomain inhibitor 2
  • HY-162892
    BRD4-IN-9
    		Inhibitor
    BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model.
    BRD4-IN-9
  • HY-144318
    CREB-IN-1 TFA
    		Inhibitor
    CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.
    CREB-IN-1 TFA
  • HY-161881
    SMARCA2-IN-9
    		Inhibitor
    SMARCA2-IN-9 (compound 11) is a SMARCA2, PBRM1 bromodomains 2 (PBRM1(2)), and PBRM1 bromodomains 5 (PBRM1(5)) inhibitor with Kd values of 1.6 μM, 2.5 μM, and 3.95 μM, respectively.
    SMARCA2-IN-9
  • HY-179684
    PCC0105005
    		Inhibitor
    PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine.
    PCC0105005
  • HY-159460
    PROTAC SMARCA2/4-degrader-8
    		Inhibitor
    PROTAC SMARCA2/4-degrader-8 (Compound I-502) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-8 degrades SMARCA2 with DC50 <100 nM in A549 and in MV411, degrades SMARCA4 with DC50<100 nM in MV411(Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W063924); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-8
  • HY-177927
    CBP-IN-1 acid
    		Inhibitor
    CBP-IN-1 acid is a CBP Inhibitor-Linker Conjugate composed of CBP-IN-1 (HY-153948) and a linker. CBP-IN-1 acid can be used to synthesize PROTACs, such as CBPD-268 (HY-161369).
    CBP-IN-1 acid
  • HY-148367A
    (1s,4s)-Menin-MLL inhibitor-23
    		Inhibitor
    (1s,4s)-Menin-MLL inhibitor-23 is the enantiomer of Menin-MLL inhibitor-23 (HY-148367). Menin-MLL inhibitor-23 (Example 99A) is a menin-MLL interaction inhibitor.
    (1s,4s)-Menin-MLL inhibitor-23
  • HY-147375
    Bromodomain inhibitor-10
    		Inhibitor
    Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40.
    Bromodomain inhibitor-10
  • HY-163160
    BET-IN-23
    		Inhibitor
    Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro.
    BET-IN-23
  • HY-180804
    CZL-077
    		Inhibitor
    CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.
    CZL-077
  • HY-155078
    BRD4 Inhibitor-27
    		Inhibitor
    BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer.
    BRD4 Inhibitor-27
  • HY-168148S
    CZL-046
    		Inhibitor
    CZL-046 (compund 29) is an oral p300 bromodomain inhibitor.
    CZL-046
  • HY-181505
    BRD4-IN-12
    		Inhibitor
    BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).
    BRD4-IN-12
  • HY-114205
    TP-238
    		Inhibitor
    TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases.
    TP-238
  • HY-178484
    BRM/BRG1 ATP-IN-6
    		Inhibitor
    BRM/BRG1 ATP-IN-6 (Compound 105) is a BRG1/BRM inhibitor. BRM/BRG1 ATP-IN-6 acts on the BAF complex, which is involved in chromatin regulation and gene expression via ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-6 demonstrates anti-tumor potential, particularly in cancers associated with BAF complex disorders.
    BRM/BRG1 ATP-IN-6
  • HY-N2020R
    Anacardic Acid (Standard)
    		Inhibitor
    Anacardic Acid (Standard) is the analytical standard of Anacardic Acid. This product is intended for research and analytical applications. Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ～8.5 μM and ～5 μM, respectively.
    Anacardic Acid (Standard)
  • HY-116237
    CREBBP-IN-9
    		Inhibitor
    CREBBP-IN-9 (Compound 9) is an inhibitor for CREBBP with an Kd of 29 μM.
    CREBBP-IN-9
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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