1. Signaling Pathways
  2. Epigenetics
  3. Histone Acetyltransferase

Histone Acetyltransferase

HATs; HAT

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-141894
    5-Ph-IAA-AM
    Activator 99.04%
    5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA (HY-134653) analog which contains an acetoxymethyl (AM) group. 5-Ph-IAA-AM affords an enhanced protein degradation in laid embryos. 5-Ph-IAA-AM can be used to disclosure the roles of proteins in C. elegans, in particular those that are involved in embryogenesis and development, through temporally controlled protein degradation.
    5-Ph-IAA-AM
  • HY-19999A
    PF-CBP1 hydrochloride
    Inhibitor 99.96%
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with?IC50?of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β,?IL-6?and?IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates?RGS4?expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
    PF-CBP1 hydrochloride
  • HY-19541
    I-CBP112
    Activator 98.20%
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
    I-CBP112
  • HY-153444
    Prifetrastat
    Inhibitor 99.75%
    KAT6-IN-1 (compound E) is a potent inhibitor of histone acetyltransferases KAT6A and KAT6B. KAT6-IN-1 can be used in cancer research.
    Prifetrastat
  • HY-154984
    JET-209
    Degrader 98.07%
    JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 contains Lenalidomide (HY-A0003) (the cereblon ligand), a linker and GNE-207 (HY-120028) (bromodomain Inhibitor). JET-209 is used for cancer research.
    JET-209
  • HY-120028
    GNE-207
    Inhibitor 99.94%
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
    GNE-207
  • HY-123604A
    TH1834 dihydrochloride
    Inhibitor 99.68%
    TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
    TH1834 dihydrochloride
  • HY-100671
    L002
    Inhibitor 99.44%
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.
    L002
  • HY-147894
    PCAF-IN-1
    Inhibitor ≥98.0%
    PCAF-IN-1 is a highly selective PCAF inhibitor. PCAF-IN-1 is a antitumor agents, which can be used in tumor research research.
    PCAF-IN-1
  • HY-66005S
    Acetaminophen-d4
    99.60%
    Acetaminophen-d4 is the deuterium 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[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
    Acetaminophen-d<sub>4</sub>
  • HY-100734
    Histone Acetyltransferase Inhibitor II
    Inhibitor 99.01%
    Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
    Histone Acetyltransferase Inhibitor II
  • HY-N2345
    Procyanidin B3
    Inhibitor 99.92%
    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
  • HY-153604
    MC4171
    Inhibitor 98.68%
    MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer.
    MC4171
  • HY-128876
    CBP/p300-IN-3
    Inhibitor 98.95%
    CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
    CBP/p300-IN-3
  • HY-158113
    CBPD-409
    Degrader
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker).
    CBPD-409
  • 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-147288
    NSC 694621
    Inhibitor 99.01%
    NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 µM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells.
    NSC 694621
  • HY-159099
    HbF inducer 2
    Degrader 99.15%
    HbF inducer 3 (Compound dWIZ-2) is an orally active molecular glue, which degrades the WIZ transcription factor (DC50=13 nM in primary human erythroid precursor cell) and induces the expression of fetal hemoglobin (HbF) (EC50=100 nM). HbF inducer 3 exhibits good pharmacokinetic characteristics in cynomolgus monkeys.
    HbF inducer 2
  • HY-16531A
    YF-2 hydrochloride
    Activator 99.61%
    YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
    YF-2 hydrochloride
  • HY-147895
    PCAF-IN-2
    Inhibitor ≥98.0%
    PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase.
    PCAF-IN-2
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