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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-142520
    I-BET567
    		Inhibitor 99.49%
    I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
    I-BET567
  • HY-139707
    Thalidomide-NH-CBP/p300 ligand 2
    		Degrader 98.55%
    Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based CBP and p300 degrader (extracted from patent WO2020173440).
    Thalidomide-NH-CBP/p300 ligand 2
  • HY-112398
    GSK1379725A
    		98.12%
    GSK1379725A is a selective BPTF ligand with a Kd of 2.8 uM, showing no binding activity for Brd4.
    GSK1379725A
  • HY-151529
    PBRM1-BD2-IN-2
    		Inhibitor ≥99.0%
    PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer.
    PBRM1-BD2-IN-2
  • HY-13032A
    GSK 525768A
    		Control 99.68%
    GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
    GSK 525768A
  • HY-151812
    CBP/p300-IN-20
    		Inhibitor 98.03%
    CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.
    CBP/p300-IN-20
  • HY-156568A
    SMD-3040 TFA
    		Degrader 99.90%
    SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 TFA
  • HY-N3213
    Naringenin triacetate
    		99.65%
    Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1).
    Naringenin triacetate
  • HY-N6901
    Luteolin 7-sulfate
    Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
    Luteolin 7-sulfate
  • HY-147202
    BRD4 Inhibitor-24
    		Inhibitor 99.27%
    BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A).
    BRD4 Inhibitor-24
  • HY-156273
    HDAC/JAK/BRD4-IN-1
    		Inhibitor
    HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo.
    HDAC/JAK/BRD4-IN-1
  • HY-100696
    PNZ5
    		Inhibitor 99.61%
    PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).
    PNZ5
  • HY-110215
    XD14
    		Inhibitor
    XD14 is a potent BET inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with Kds of 170, 380, and 160 nM, respectively.
    XD14
  • HY-104067
    Naphthol AS-MX phosphate
    		Inhibitor 99.50%
    Naphthol AS-MX phosphate (NASTRp) is a small molecule inhibitor of the CREB (cyclic adenosine phosphate reaction element binding protein)-CBP (CREB binding protein) transcription factor complex. Naphthol AS-MX phosphate shows antitumor activity against lung cancer cells, inhibiting tumor cell proliferation (IC50=3.701 μmol/L), colony formation, and anchored independent growth in soft AGAR. Naphthol AS-MX phosphate can be used in the study of KRAS mutated lung cancer, especially for KRAS mutated lung cancer with poor chemotherapy resistance and prognosis.
    Naphthol AS-MX phosphate
  • HY-101125B
    D-Moses
    		Control
    D-Moses (D-45) is an enantiomer of L-Moses (HY-101125). L-Moses (L-45) is a potent and selective p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor. D-Moses shows no observable binding for PCAF Brd. D-Moses can be used as an inactive control compound to L-Moses.
    D-Moses
  • HY-150211
    DC-BPi-03
    		Inhibitor 99.77%
    DC-BPi-03 is a potent BPTF-BRD inhibitor with an IC50 of 698.3 nM and a Kd of 2.81 μM.
    DC-BPi-03
  • HY-163729
    I-BET787
    		Inhibitor 99.88%
    I-BET787 is a orally active BET bromine domain inhibitor with pIC50s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice.
    I-BET787
  • HY-103297
    OXFBD02
    		Inhibitor 98.04%
    OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM.
    OXFBD02
  • HY-161651A
    BRD4 ligand 6 TFA
    		99.79%
    BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6 (HY-161651). BRD4 ligand 6 TFA is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650).
    BRD4 ligand 6 TFA
  • HY-12421
    BET-BAY 002
    		Inhibitor 99.80%
    BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
    BET-BAY 002
Cat. No. Product Name / Synonyms Application Reactivity