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-N2345R
    Procyanidin B3 (Standard)
    		Inhibitor
    Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
    Procyanidin B3 (Standard)
  • HY-147261
    B026
    		Inhibitor
    B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.
    B026
  • HY-11055
    KP 544
    KP 544 is a potent neurotrophic protein enhancer that amplifies nerve growth factor (NGF)-induced neurite outgrowth of PC12 cells and SH-SY5Y neuroblastoma cells. KP544 also enhances choline acetyltransferase activity. KP 544 selectively interact in the differentiation pathway downstream of MAPK in a manner that amplifies nerve growth factor and cyclic AMP effects and is also neuroprotective.
    KP 544
  • HY-162128
    Antitumor agent-130
    		Inhibitor
    Antitumor agent-130 (Compound 7b) is a p300 histone acetyltransferases (HAT) inhibitor with an IC50 of 1.51 μM. Antitumor agent-130 combinates with doxorubicin (HY-15142A) can significantly inhibit tumor growth and invasion in vitro and in vivo.
    Antitumor agent-130
  • HY-162994
    KAT6A-IN-1
    		Inhibitor
    KAT6A-IN-1 (compund 5) is a KAT6A inhibitor.
    KAT6A-IN-1
  • HY-RS07083
    KAT7 Human Pre-designed siRNA Set A
    		Inhibitor

    KAT7 Human Pre-designed siRNA Set A contains three designed siRNAs for KAT7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    KAT7 Human Pre-designed siRNA Set A
  • HY-174866
    BT-O2C
    		Inhibitor
    BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).
    BT-O2C
  • HY-128363
    Ep300/CREBBP-IN-2
    		Inhibitor
    Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer.
    Ep300/CREBBP-IN-2
  • HY-143441
    CBP/p300-IN-17
    		Inhibitor
    CBP/p300-IN-17 (compound 7) is a potent EP300/CBP HAT inhibitor with IC50s of 0.18, 0.69 µM for HAT EP300 and LK2 H3K27, respectively.
    CBP/p300-IN-17
  • HY-177045
    KAT6A/KAT7-IN-3
    		Inhibitor
    KAT6A/KAT7-IN-3 (Example 191) is a KAT6A and KAT7 inhibitor. The IC50 of KAT6A/KAT7-IN-3 for KAT6A is ≤ 50 nM and > 10 nM, while the IC50 for KAT7 is ≤ 1 nM. KAT6A/KAT7-IN-3 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-3 also inhibits tumor cell proliferation, with an IC50 of > 2 μM and ≤ 5 μM for CAMA-1. KAT6A/KAT7-IN-3 can be used in the study of cancer.
    KAT6A/KAT7-IN-3
  • HY-147289
    NSC 698600
    		Inhibitor
    NSC 698600 is a potent PCAF inhibitor, with IC50 of 6.51 µM (PCAF/H31-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells.
    NSC 698600
  • HY-66005S3
    Acetaminophen-13C6
    Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
    Acetaminophen-<sup>13</sup>C<sub>6</sub>
  • 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-168201
    MJP6412
    		Degrader
    MJP6412 is a potent degrader histone acetyltransferases p300/CBP, with DC50 of 1.6 and 1.2 nM for p300 and CBP, respectively. MJP6412 plays an important role in cancer research.
    MJP6412
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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