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-141466A
    Crotonyl-CoA tetrasodium
    		Substrate
    Crotonyl-CoA tetrasodium, a high-energy acyl donor, is an intermediate in the fermentation of butyric acid, and in the metabolism of lysine and tryptophan. Crotonyl-CoA tetrasodium is important in the metabolism of fatty acids and amino acids. Crotonyl-CoA tetrasodium acts as a substrate for p300’s histone crotonyltransferase activity, competing with acetyl-CoA for p300-mediated histone acylation reactions. Crotonyl-CoA tetrasodium regulates global and gene-specific histone crotonylation levels in cells, with cellular concentration changes altering histone crotonylation at regulatory elements of activated genes. Crotonyl-CoA tetrasodium serves as the substrate for crotonyl-CoA reductase/carboxylase (CCRC)-catalyzed NADPH-mediated reduction and carbon dioxide trapping to form unusual alkylmalonyl-CoA polyketide synthase extender units. Crotonyl-CoA tetrasodium can be used for the research of LPS-induced inflammatory response.
    Crotonyl-CoA tetrasodium
  • HY-100697
    TPOP146
    		Inhibitor 98.94%
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
    TPOP146
  • HY-139108
    DCH36_06
    		Inhibitor 99.19%
    DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
    DCH36_06
  • HY-114566
    SPV106
    		Activator 98.59%
    SPV106 is histone acetylase (HAT) and GCN5-related N-acetyltransferases (GNAT) activator. SPV106 can be used for the research of type 2 diabetes (T2D).
    SPV106
  • HY-112610
    CF53
    		Inhibitor 99.81%
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
    CF53
  • HY-147290
    NSC 694623
    		Inhibitor 99.53%
    NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer.
    NSC 694623
  • HY-161483
    CBP/p300 ligand 3
    		Inhibitor 98.82%
    CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function.
    CBP/p300 ligand 3
  • HY-169955A
    WIZ degrader 8 TFA
    		Degrader 99.41%
    WIZ degrader 8 (TFA) is the trifluoroacetic acid of WIZ degrader 8 (HY-169955). WIZ degrader 8 (compound 10) is a potent and selective degrader of the transcription factor WIZ, which can potently induce HbF expression. WIZ degrader 8 can lead to WIZ degradation and induce HbF expression, and has the potential to be an inhibitor of sickle cell disease.
    WIZ degrader 8 TFA
  • HY-132197
    CBP/p300-IN-12
    		Inhibitor 99.72%
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
    CBP/p300-IN-12
  • HY-168428
    CHI-KAT8i5
    		Inhibitor 98.00%
    CHI-KAT8i5 is a selective and orally active KAT8 inhibitor with a KD value of 19.72 μM. CHI-KAT8i5 does not bind to other proteins in HAT family (KAT2A, KAT2B, KAT5, and KAT7). CHI-KAT8i5 induces cancer cell apoptosis. CHI-KAT8i5 suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway.
    CHI-KAT8i5
  • HY-120290
    PU141
    		Inhibitor 99.96%
    PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
    PU141
  • HY-104068
    Naphthol AS-E
    		Inhibitor 98.0%
    Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 μM. Naphthol AS-E can be used for cancer research.
    Naphthol AS-E
  • HY-111954
    (+)-Erinacin A
    		99.81%
    (+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage.
    (+)-Erinacin A
  • HY-102059
    MOZ-IN-2
    		Inhibitor 99.58%
    MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC50 of 125 μM.
    MOZ-IN-2
  • HY-141546
    Pocenbrodib
    		Inhibitor 98.49%
    Pocenbrodib is a P300/CBP inhibitor. Pocenbrodib blocks the function of P300/CBP and inhibits the acetylation of histones and non-histone proteins. Pocenbrodib may be used in research related to castration-resistant prostate cancer and other cancers.
    Pocenbrodib
  • HY-159098
    dWIZ-1
    		Degrader
    dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease.
    dWIZ-1
  • HY-169955
    WIZ degrader 8
    		Degrader 98.30%
    WIZ degrader 8 (compound 10) is a potent and selective degrader of the transcription factor WIZ, which can potently induce HbF expression. WIZ degrader 8 can lead to WIZ degradation and induce HbF expression, and has the potential to be an inhibitor of sickle cell disease.
    WIZ degrader 8
  • HY-178486
    SH6
    		99.43%
    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-120317
    CPTH2-Alkyne
    		Inhibitor 99.9%
    CPTH2-Alkyne is a cell active analog of CPTH2 (HY-W013274). CPTH2-Alkyne specifically accumulates in nucleoli and locates in nuclear periphery and in cytoplasma. CPTH2-Alkyne inhibits N-acetyltransferase 10 (NAT10). CPTH2-Alkyne is used in study of nuclear architecture and application in laminopathy.
    CPTH2-Alkyne
  • HY-146277A
    CBP/p300-IN-19 hydrochloride
    		Inhibitor 99.00%
    CBP/p300-IN-19 hydrochloride is a potent and selective 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 hydrochloride shows antitumor activity.
    CBP/p300-IN-19 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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