2. Signaling Pathways
  3. Epigenetics
  4. Histone Acetyltransferase

Histone Acetyltransferase

HATs; HAT

Histone Acetyltransferase

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Histone acetyltransferases (HATs) are epigenetic enzymes that install acetyl groups onto lysine residues of cellular proteins such as histones, transcription factors, nuclear receptors, and enzymes. HATs are crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells. HATs have been shown to play a role in diseases ranging from cancer and inflammatory diseases to neurological disorders, both through acetylations of histone proteins and non-histone proteins.

HATs can be grouped into at least five different subfamilies (HAT1, Gcn5/PCAF, MYST, p300/CBP, and Rtt109). HATs mediate many different biological processes including cell-cycle progression, dosage compensation, repair of DNA damage, and hormone signaling. Aberrant HAT function is correlated with several human diseases including solid tumors, leukemias, inflammatory lung disease, viral infection, diabetes, fungal infection, and drug addiction.

Histone Acetyltransferase Isoform Specific Products:

Histone Acetyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-174868
    iP300w
    		Inhibitor
    iP300w (Compound 9) is a Histone acetyltransferase p300 (KAT3B) inhibitor. iP300w can be used for synthesis of PROTAC BT-O2C (HY-174866).
    iP300w
  • HY-175180
    Conophyllidine
    		Inhibitor
    Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs.
    Conophyllidine
  • HY-162995
    KAT6A-IN-2
    		Inhibitor
    KAT6A-IN-2 (compund 7) is a KAT6A inhibitor.
    KAT6A-IN-2
  • HY-138945
    SYY-B085-1
    		Inhibitor
    SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor extracted from patent WO2019201291A1.
    SYY-B085-1
  • HY-161710
    XYD129
    		Degrader
    XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)).
    XYD129
  • HY-162997
    KAT6-IN-3
    		Inhibitor
    KAT6-IN-3 (compund 10) competitively targets KAT6A and KAT6B.
    KAT6-IN-3
  • HY-178486
    SH6
    		Inhibitor
    SH6 is a transcription factor ZBTB7A degrader. SH6 is promising for research of β-hemoglobinopathies such as sickle cell disease (SCD) and β-thalassemia.
    SH6
  • HY-173641
    MNN-02-155
    MNN-02-155 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. MNN-02-155 induces potent activation of the BCL6-target reporter gene and cell death. MNN-02-155 can be used for the study of diffuse large B cell lymphomas (DLBCLs).
    MNN-02-155
  • HY-162921
    KAT6-IN-2
    		Inhibitor
    KAT6-IN-2 (Compound 25) is a potent KAT6 inhibitor. KAT6-IN-2 is promising for research of cancers.
    KAT6-IN-2
  • HY-163819
    WIZ degrader 3
    		Degrader
    WIZ degrader 3 (Compound 29) is a degrader for widely interspaced zinc finger motifs (WIZ), with an AC50 of 6.4 nM. WIZ degrader 3 induces the expression of fetal hemoglobin (HbF), with an EC50 of 45 nM. WIZ degrader 3 can be used for the research of blood disorders, such as sickle cell disease and β- thalassemia.
    WIZ degrader 3
  • 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-177445
    KAT6-IN-4
    		Inhibitor
    KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER+/HER2- breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC).
    KAT6-IN-4
  • HY-122822
    GSK699
    		Degrader
    GSK699 is a PCAF/GCN5 PROTAC degrader. GSK699 promotes the ubiquitination and degradation of PCAF/GCN5. GSK699 inhibits the production of cytokines/chemokines (e.g., IL-6, CXCL1/GROα). GSK699 can be used in the research of inflammatory diseases (target protein ligand: HY-101027, CRBN ligand: HY-103596).
    GSK699
  • HY-103669
    HAT-IN-1
    		Inhibitor
    HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
    HAT-IN-1
  • HY-139149A
    (E/Z)-NiCur
    (E/Z)-NiCur is the active isomer of NiCur (HY-139149). (E/Z)-NiCur is a potent CBP histone acetyltransferase (HAT) inhibitor.
    (E/Z)-NiCur
  • HY-128362
    Ep300/CREBBP-IN-8
    		Inhibitor
    Ep300/CREBBP-IN-8 (Example 37) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.014 and 0.018 μM, respectively. Ep300/CREBBP-IN-8 can be used for the research of cancer.
    Ep300/CREBBP-IN-8
  • HY-159587
    P300-IN-4
    		Inhibitor
    P300-IN-4 (compound 6) is a (p300) inhibitor with the IC50 of 12.2 μM.
    P300-IN-4
  • HY-176251
    CBP/p300-IN-22
    		Inhibitor
    CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC50 of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.
    CBP/p300-IN-22
  • HY-RS07080
    KAT5 Human Pre-designed siRNA Set A
    		Inhibitor

    KAT5 Human Pre-designed siRNA Set A contains three designed siRNAs for KAT5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    KAT5 Human Pre-designed siRNA Set A
  • HY-146277
    CBP/p300-IN-19
    		Inhibitor
    CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity.
    CBP/p300-IN-19
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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