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-128364
    Ep300/CREBBP-IN-3
    		Inhibitor
    Ep300/CREBBP-IN-3 (Example 61) is a potent Ep300 and CREBBP inhibitor with IC50s of 0.056 and 0.095 μM, respectively. Ep300/CREBBP-IN-3 can be used for the research of cancer.
    Ep300/CREBBP-IN-3
  • 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-177043
    KAT6A/KAT7-IN-1
    		Inhibitor
    KAT6A/KAT7-IN-1 is a KAT6A and KAT7 inhibitor with IC50 for KAT6A of within the range of 1-10 nM, and for KAT7 of ≤ 1 nM. KAT6A/KAT7-IN-1 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-1 can be used in the research of breast adenocarcinoma.
    KAT6A/KAT7-IN-1
  • HY-181758
    PROTAC CBP/p300/BRD4 Degrader-1
    		Degrader
    PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer.
    PROTAC CBP/p300/BRD4 Degrader-1
  • HY-143440
    CBP/p300-IN-16
    		Inhibitor
    CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC50s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively.
    CBP/p300-IN-16
  • HY-181261
    PROTAC CBP/P300 Degrader-2
    PROTAC CBP/P300 Degrader-2 (compound 2) is a PROTAC-based CBP/P300 degrader that can be used in the research of cancer, autoimmune, inflammatory, and neurodegenerative diseases.
    PROTAC CBP/P300 Degrader-2
  • HY-P11551
    Histone H4 peptide
    Histone H4 peptide is a peptide that interacts with hNatD. Histone H4 peptide exhibits polar interactions with hNatD. Histone H4 peptide can be used in lung cancer research.
    Histone H4 peptide
  • HY-121089
    P300-IN-5
    		Inhibitor
    P300-IN-5 is a biological inhibitor that demonstrates potent activity against histone acetyltransferases (HAT) both in vitro and in vivo. P300-IN-5 may serve as an alternative therapeutic agent, especially in contexts requiring caution, such as during breastfeeding.
    P300-IN-5
  • HY-164005
    CBP/EP300 bromodomain receptor-IN-1
    		Inhibitor
    CBP/EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor for CBP/EP300 bromodomain receptor, which binds to proteins having a bromodomain in nanomolar level.
    CBP/EP300 bromodomain receptor-IN-1
  • HY-183802
    PROTAC CBP/P300 Degrader-4
    		Degrader
    PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC50 of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies.
    PROTAC CBP/P300 Degrader-4
  • 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-181843
    HDAC-IN-99
    		Activator
    HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.
    HDAC-IN-99
  • 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-178360
    NP1192
    		Degrader
    NP1192 is a potent, selective PROTAC NAT10 degrader that depletes NAT10 protein and inhibits ac4C modification in cancer cells. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research. (Blue: CRBN ligand (HY-148834); Black: linker; Pink: NAT10 ligand (HY-16706)).
    NP1192
  • HY-181279
    PCAF/GCN5 ligand 1
    PCAF/GCN5 ligand 1 is a PCAF/GCN5 ligand with high binding affinity. PCAF/GCN5 ligand 1 shows no functional effect on PCAF/GCN5 activity. PCAF/GCN5 ligand 1 undergoes optimization into a potent and selective PCAF/GCN5 ligand GSK4027 (HY-101027).
    PCAF/GCN5 ligand 1
  • 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 is a KAT6A inhibitor with an IC50 of <10 μM. KAT6A-IN-1 can be used for the research of cancer.
    KAT6A-IN-1
  • HY-181759
    CBP/p300/BRD4 ligand-1
    		Ligand
    CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers.
    CBP/p300/BRD4 ligand-1
  • HY-P11829
    ACTR-AD1 2L
    		Inhibitor
    ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer.
    ACTR-AD1 2L
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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