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-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-186064
    CBP/p300 ligand-Linker Conjugate 3
    CBP/p300 ligand-Linker Conjugate 3 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CBP/p300 and a PROTAC linker, which recruits E3 ligases. CBP/p300 ligand-Linker Conjugate 3 can be used for synthesis of PROTAC CBP/P300 Degrader-2 (HY-181261).
    CBP/p300 ligand-Linker Conjugate 3
  • HY-181695
    PROTAC KAT2A/B degrader-1
    		Degrader
    PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance.
    PROTAC KAT2A/B degrader-1
  • HY-185009
    GSK702
    		Degrader
    GSK702, a PROTAC, is a the less active cis-(S,S)-enantiomer of GSK983 (P300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) PROTAC). GSK702 induces only a small decrease of PCAF protein levels. GSK702 binds to CRBN and causes a reduction of IL-1β in macrophages. GSK702 can be used for the study of inflammatory mediators.
    GSK702
  • HY-183256
    BAY-7728
    		Inhibitor
    BAY-7728 is an orally active and selective dual inhibitor of KAT6A (IC50: 45 nM)/KAT6B (IC50: 95 nM). BAY-7728 can effectively inhibit tumor growth and regulate the acetylation level of histone H3K23. BAY-7728 can be used for tumor research.
    BAY-7728
  • 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-W197205
    SL010110
    		Activator
    SL010110 is an anti-hyperglycemic agent. SL010110 potently inhibits gluconeogenesis by inhibiting SIRT2, activating p300, and subsequently promoting PEPCK1 degradation. SL010110 downregulates the protein level of PEPCK1 without affecting the gene expressions of PEPCK, glucose-6-phosphatase, and fructose-1,6-bisphosphatase. SL010110 significantly improves glucose homeostasis in type 2 diabetic (T2D) mice model. SL010110 can be used for T2D research.
    SL010110
  • HY-181669
    P300-IN-6
    		Inhibitor
    P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma.
    P300-IN-6
  • 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-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-181854
    ZX079
    		Inhibitor
    ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.
    ZX079
  • 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-181852
    CBP/p300 ligand 10
    		Degrader
    CBP/p300 ligand 10 (Compound 3-E) is a CBP/p300 degrader. CBP/p300 ligand 10 also serves as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) and can be used to synthesize the PROTAC CBP/p300 Degrader-2 (HY-181261).
    CBP/p300 ligand 10
  • 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-114510
    PRMT/HKMT-IN-1
    		Inhibitor
    PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia.
    PRMT/HKMT-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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