2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain

Related Products

PDF 3.95 MB

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-157814
    Menin-MLL inhibitor-25
    		Inhibitor
    Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest.
    Menin-MLL inhibitor-25
  • HY-181690
    Menin-MLL-IN-37
    		Inhibitor
    Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC50 of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML).
    Menin-MLL-IN-37
  • HY-182958
    Hsp70TAC BRD4 Degrader-1
    		Degrader
    Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)).
    Hsp70TAC BRD4 Degrader-1
  • HY-183273
    BRD4/AKT-IN-1
    		Inhibitor
    BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC50 66.12 nM and AKT1 IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.
    BRD4/AKT-IN-1
  • HY-142953
    UNC6349 (Ket2)
    		Inhibitor
    UNC6349 (Ket2), a diethyllysine (Ket2)-containing ligand, binds to wild-type CBX5, with a KD of 3.2 μM.
    UNC6349 (Ket2)
  • HY-146739
    BRD4 Inhibitor-19
    		Inhibitor
    BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research.
    BRD4 Inhibitor-19
  • HY-168628
    BET-IN-27
    		Inhibitor
    BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity.
    BET-IN-27
  • HY-170390
    AB3067
    		Degrader
    AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM. (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))
    AB3067
  • HY-180428
    BRM/BRG1 ATP degrader-1
    		Degrader
    BRM/BRG1 ATP degrader-1 (Compound 1) is a BRG1/BRM degrader with IC50 values for the degradation of BRM IF and BRG1 IF of 0.01-0.1 μM and > 0.1 μM respectively. BRM/BRG1 ATP degrader-1 can be used for cancer research.
    BRM/BRG1 ATP degrader-1
  • HY-169861
    PROTAC SMARCA2/4 degrader-37
    		Degrader
    PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC-based SMARCA2/4 degrader, with an IC50 of ≤0.1 μM (Pink: SMARCA2/4 lignad (HY-172446); Black: CRBN ligand (HY-41547); Linker (HY-N2407)).
    PROTAC SMARCA2/4 degrader-37
  • HY-N12378A
    α-Patchoulene
    		Inhibitor
    α-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. α-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. α-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. α-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma.
    α-Patchoulene
  • HY-123626
    BiBET
    BiBET is a chemical probe of BET/BRD4 and is able to bind to two bromodomains simultaneously in a bivalent and cis-binding mode.
    BiBET
  • HY-16652R
    Apabetalone (Standard)
    		Inhibitor
    Apabetalone (Standard) is the analytical standard of Apabetalone. This product is intended for research and analytical applications. Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively.
    Apabetalone (Standard)
  • HY-101027R
    GSK 4027 (Standard)
    		Inhibitor
    GSK 4027 (Standard) is the analytical standard of GSK 4027 (HY-101027). This product is intended for research and analytical applications. GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK 4027 (Standard)
  • HY-176070
    HRG038
    		Inhibitor
    HRG038 is a selective covalent BRD4 degrader. HRG038 binds covalently to the E3 ubiquitin ligase CUL4 DCAF16, recruiting it to BRD4, leading to the ubiquitination and subsequent proteasomal degradation of BRD4. HRG038 is promising for research of cancers.
    HRG038
  • HY-101567R
    BMS-986158 (Standard)
    		Inhibitor
    BMS-986158 (Standard) is the analytical standard of BMS-986158 (HY-101567). This product is intended for research and analytical applications. BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
    BMS-986158 (Standard)
  • HY-101146R
    SF2523 (Standard)
    		Inhibitor
    SF2523 (Standard) is the analytical standard of SF2523 (HY-101146). This product is intended for research and analytical applications. SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
    SF2523 (Standard)
  • HY-101084R
    NSC 228155 (Standard)
    		Inhibitor
    NSC 228155 (Standard) is the analytical standard of NSC 228155 (HY-101084). This product is intended for research and analytical applications. NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
    NSC 228155 (Standard)
  • HY-15743R
    Birabresib (Standard)
    		Inhibitor
    Birabresib (Standard) is the analytical standard of Birabresib. This product is intended for research and analytical applications. Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
    Birabresib (Standard)
  • HY-100972R
    ARV-771 (Standard)
    		Inhibitor
    ARV-771 (Standard) is the analytical standard of ARV-771 (HY-100972). This product is intended for research and analytical applications. ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
    ARV-771 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.