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-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-100734
    Histone Acetyltransferase Inhibitor II
    		Inhibitor 98.70%
    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-147894
    PCAF-IN-1
    		Inhibitor 98.45%
    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-173552
    TCIP3
    		Inhibitor 99.30%
    TCIP3 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. TCIP3 redirects p300 and CBP to activate programmed cell death genes normally repressed by the oncogenic driver, BCL6. TCIP3 can be used for the study of diffuse large B cell lymphomas (DLBCLs). TCIP3 exhibits no toxicity in non-transformed tonsillar lymphocytes or fibroblasts.
    TCIP3
  • HY-122822
    GSK699
    		Degrader 98.80%
    GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases.
    GSK699
  • HY-101027A
    GSK4028
    		98.06%
    GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK4028
  • HY-152241
    DS-9300
    		Inhibitor 99.83%
    DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.
    DS-9300
  • HY-176244
    KI-TOX-A3
    		Inhibitor 99.15%
    KI-TOX-A3 is a TOX protein-protein interaction inhibitor that blocks the TOX-KAT7 protein-protein interaction with an IC50 of 0.51 μM. KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses exhaustion of CD8+ T cells, and inhibits the proliferation of T cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 shows promise for use in studies of hematological malignancies such as T-ALL.
    KI-TOX-A3
  • HY-19763
    Ifupinostat
    		99.30%
    Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research.
    Ifupinostat
  • HY-N0005S
    Curcumin-d6
    		Inhibitor 99.78%
    Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d<sub>6</sub>
  • 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-128876
    CBP/p300-IN-3
    		Inhibitor 98.01%
    CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
    CBP/p300-IN-3
  • HY-147288
    NSC 694621
    		Inhibitor 98.67%
    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-131035
    Lys-CoA TFA
    		Inhibitor 98.52%
    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-W019670R
    N4-Acetylcytidine (Standard)
    N4-acetylcytidine (N4A) is an endogenous nucleoside metabolite from the degradation of tRNA. N4-Acetylcytidine is formed by N-acetyltransferase 10 and other enzymes. N4-acetylcytidine might sustain NLRP3 inflammasome activation via induction of HMGB1 expression and releasee. N4-Acetylcytidine modifies mRNA, tRNA and rRNA, affecting their stability, translation efficiency (such as enterovirus 71 RNA). N4-Acetylcytidine is used in the study of cancer, neuroinflammatory diseases, viral infections and obesity.
    N4-Acetylcytidine (Standard)
  • HY-16531A
    YF-2 hydrochloride
    		Activator 99.29%
    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-149470
    MOZ-IN-3
    		Inhibitor 98.75%
    MOZ-IN-3 (Compound 6j) is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). MOZ-IN-3 has antitumor activity against four different myeloid leukemia cell lines (HL-60, U937, SKNO-1, K562). MOZ-IN-3 has favorable metabolic stability and pharmacokinetics.
    MOZ-IN-3
  • HY-115539
    Windorphen
    		Inhibitor 99.75%
    Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP.
    Windorphen
  • HY-161875
    NAT1-IN-1
    		Inhibitor 99.77%
    NAT1-IN-1 (compound 350) is a potent N-acetyltransferase 1 (NAT1)-targeted inhibitor, with an IC50 of 44 nM. NAT1-IN-1 can be used for the research of hypermetabolic diseases such as amyotrophic lateral sclerosis, cancer cachexia, and sepsis.
    NAT1-IN-1
  • HY-66005S2
    Acetaminophen-d7
    		99.92%
    Acetaminophen-d7 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. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
    Acetaminophen-d<sub>7</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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