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-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-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-120028
    GNE-207
    		Inhibitor
    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-100726
    GNE-272
    		Inhibitor 99.76%
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
    GNE-272
  • 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-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-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-153444
    KAT6-IN-1
    		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.
    KAT6-IN-1
  • HY-132197
    CBP/p300-IN-12
    		Inhibitor 99.70%
    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-N2345
    Procyanidin B3
    		Inhibitor 99.63%
    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-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-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-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
  • 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-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-131035
    Lys-CoA TFA
    		Inhibitor 99.42%
    Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.
    Lys-CoA TFA
  • HY-100697
    TPOP146
    		Inhibitor 98.98%
    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-128875
    CBP/p300-IN-10
    		Inhibitor 98.69%
    CBP/p300-IN-10 is a highly potent histone acetyltransferase EP300 and CREBBP with IC50 values of 26 nM and 39 nM, respectively. CBP/p300-IN-10 can be used to research anticancer.
    CBP/p300-IN-10
  • HY-112610
    CF53
    		Inhibitor 99.78%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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