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-169272
    PROTAC SMARCA2 degrader-21
    		Degrader
    PROTAC SMARCA2 degrader-21 (Compound I-5) is a PROTAC degrader for SMARCA, that degrades SMARCA2 with a DC50 of 10-50 nM in A549 cell, and degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <1 nM and >100 nM, respectively.
    PROTAC SMARCA2 degrader-21
  • HY-153948
    CBP-IN-1
    CBP-IN-1 (compound 12) is a potent CBP inhibitor, with an IC50 of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4(1), with IC50 values of 690 and 3100 nM, respectively.
    CBP-IN-1
  • HY-141703
    DC-BPi-11
    		Inhibitor
    DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation.
    DC-BPi-11
  • HY-134921
    MI-nc dihydrochloride
    		Inhibitor
    MI-nc dihydrochloride is a weak inhibitor of the Menin-MLL fusion protein interaction with an IC50 of 193 μM. MI-nc dihydrochloride can be used as a negative control compound of MI-2.
    MI-nc dihydrochloride
  • HY-161887
    SMARCA2-IN-8
    		Inhibitor
    SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice.
    SMARCA2-IN-8
  • HY-173257
    Cath-L-dBET1
    		Degrader
    Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
    Cath-L-dBET1
  • HY-173327
    BRD4 degrader-6
    		Degrader
    BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity.
    BRD4 degrader-6
  • HY-159457
    PROTAC SMARCA2/4-degrader-6
    		Degrader
    PROTAC SMARCA2/4-degrader-6 (compound I-438) is a SMARCA2/4 degrader. PROTAC SMARCA2/4-degrader-6 has the potential for the research of cancer. (Pink: SMARCA2/4 ligand, (HY-159545); Black: linker (HY-W006635); Blue: VHL ligand (HY-112078)).
    PROTAC SMARCA2/4-degrader-6
  • HY-162240
    SJH1-51B
    		Degrader
    SJH1-51B is a potent PROTAC degrader of BRD4. SJH1-51B has anti-tumor effect.
    SJH1-51B
  • HY-168235
    (S,R,S)-AHPC-Me-amide-C9-acid
    		Degrader
    (S,R,S)-AHPC-Me-amide-C9-acid is a E3 ligase ligand-linker conjugate, used for the synthesis of PROTAC SMARCA2 degrader-31 (HY-168234).
    (S,R,S)-AHPC-Me-amide-C9-acid
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1
    		Inhibitor
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
    PROTAC BRD2/BRD4 degrader-1
  • HY-155889
    IV-275
    		Inhibitor
    IV-275 is an inhibitor of both BRG1 and BRM bromodomains. IV-275 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-275 inhibits the invasiveness of GBM cells. IV-275 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide.
    IV-275
  • HY-174811
    PROTAC BRD4 Degrader-33
    		Degrader
    PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model. Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC BRD4 Degrader-33
  • HY-156566
    PROTAC BRD4 Degrader-21
    		Inhibitor
    PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research.
    PROTAC BRD4 Degrader-21
  • HY-146445
    P300 bromodomain-IN-1
    		Inhibitor
    P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells.
    P300 bromodomain-IN-1
  • HY-170226
    BET-IN-28
    		Inhibitor
    BET-IN-28 (Compound 44) is a highly potent inhibitor of bromodomain and extra-terminal domain (BET), with an IC50 value of 4.47 nM against BRD4-BD1. BET-IN-28 blocks the interaction between BET proteins and N-acetylated lysine residues on histone tails, down-regulates certain genes. BET-IN-28 can be used for hematological malignancies and solid tumors study.
    BET-IN-28
  • HY-P10066
    Menin-MLL inhibitor 31
    		Inhibitor
    Menin-MLL inhibitor 31 (compound 18) is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM.
    Menin-MLL inhibitor 31
  • HY-161368
    BRD-SF2
    		Degrader
    BRD-SF2 is a BRD4-targeted PROTAC degrader (DC50: 17.2 μM) (Blue: VHL ligand, black: linker, pink: BRD4 ligand).
    BRD-SF2
  • HY-150684
    GXH-II-052
    		Inhibitor
    GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc.
    GXH-II-052
  • HY-151534
    PBRM1-BD2-IN-7
    		Inhibitor
    PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer.
    PBRM1-BD2-IN-7
Cat. No. Product Name / Synonyms Application Reactivity