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-W1122565
    KAT2A/B ligand 1
    		Ligand
    KAT2A/B ligand 1 (compound 32a) is a KAT2A/B ligand. KAT2A/B ligand 1 can be used as a target protein ligand for the synthesis of AUR1545 (HY-173158).
    KAT2A/B ligand 1
  • HY-123009
    KCN1
    		Inhibitor
    KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest.
    KCN1
  • HY-66005S5
    Acetaminophen-d5
    		Inhibitor
    Acetaminophen-d5 is deuterated-labeled Acetaminophen (HY-66005). 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>5</sub>
  • HY-100482R
    CPI-637 (Standard)
    		Inhibitor
    CPI-637 (Standard) is the analytical standard of CPI-637 (HY-100482). This product is intended for research and analytical applications. CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.
    CPI-637 (Standard)
  • HY-101027AR
    GSK4028 (Standard)
    GSK4028 (Standard) is the analytical standard of GSK4028 (HY-101027A). This product is intended for research and analytical applications. 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 (Standard)
  • HY-104068R
    Naphthol AS-E (Standard)
    		Inhibitor
    Naphthol AS-E (Standard) is the analytical standard of Naphthol AS-E (HY-104068). This product is intended for research and analytical applications. 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 (Standard)
  • HY-163823
    WIZ degrader 6
    		Degrader
    WIZ degrader 6 (compound 10) is a WIZ degrader with the EC50 of ＜0.01μM. WIZ degrader 6 can be used for study of sickle cell disease.
    WIZ degrader 6
  • HY-163822
    WIZ degrader 5
    		Degrader
    WIZ degrader 5 (compound 41) is a WIZ degrader and induces the degradation of WIZ with maximum degradation of 88.6% in 293T cells. WIZ degrader 5 can be used for study of sickle cell disease .
    WIZ degrader 5
  • HY-108696R
    GNE-781 (Standard)
    		Inhibitor
    GNE-781 (Standard) is the analytical standard of GNE-781 (HY-108696). This product is intended for research and analytical applications. GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.
    GNE-781 (Standard)
  • HY-N0005S1
    Curcumin-d3
    		Inhibitor
    Curcumin-d3 (Diferuloylmethane-d3 ) 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>3</sub>
  • HY-108435R
    GNE-049 (Standard)
    		Inhibitor
    GNE-049 (Standard) is the analytical standard of GNE-049 (HY-108435). This product is intended for research and analytical applications. GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
    GNE-049 (Standard)
  • HY-141466
    Crotonyl-CoA
    		Substrate
    Crotonyl-CoA, a high-energy acyl donor, is an intermediate in the fermentation of butyric acid, and in the metabolism of lysine and tryptophan. Crotonyl-CoA is important in the metabolism of fatty acids and amino acids. Crotonyl-CoA acts as a substrate for p300’s histone crotonyltransferase activity, competing with acetyl-CoA for p300-mediated histone acylation reactions. Crotonyl-CoA 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 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 can be used for the research of LPS-induced inflammatory response.
    Crotonyl-CoA
  • HY-107569R
    Garcinol (Standard)
    		Inhibitor
    Garcinol (Standard) is the analytical standard of Garcinol. This product is intended for research and analytical applications. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively. Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity.
    Garcinol (Standard)
  • HY-100726R
    GNE-272 (Standard)
    		Inhibitor
    GNE-272 (Standard) is the analytical standard of GNE-272 (HY-100726). This product is intended for research and analytical applications. 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 (Standard)
  • HY-W713313
    3,5-DMA hydrochloride
    		Ligand
    3,5-DMA (3,5-Dimethoxyamphetamine) hydrochloride is an alkylphenylamine compound primarily catalyzed by NAT2. The metabolic rate of 3,5-DMA hydrochloride is closely related to the NAT2 acetylator genotype variation. 3,5-DMA is useful for studying the role of NAT2 acetylator genotype variation in the metabolism of alkylphenylamine carcinogens.
    3,5-DMA hydrochloride
  • HY-102058R
    WM-1119 (Standard)
    		Inhibitor
    WM-1119 (Standard) is the analytical standard of WM-1119 (HY-102058). This product is intended for research and analytical applications. WM-1119, a chemical probe, is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding Kd values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.
    WM-1119 (Standard)
  • HY-100734R
    Histone Acetyltransferase Inhibitor II (Standard)
    		Inhibitor
    Histone Acetyltransferase Inhibitor II (Standard) is the analytical standard of Histone Acetyltransferase Inhibitor II (HY-100734). This product is intended for research and analytical applications. 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 (Standard)
  • HY-160260
    EP300/CBP-IN-1
    		Inhibitor
    EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC50s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells.
    EP300/CBP-IN-1
  • HY-166309
    Crotonyl-CoA tetralithium
    		Substrate
    Crotonyl-CoA tetralithium, a high-energy acyl donor, is an intermediate in the fermentation of butyric acid, and in the metabolism of lysine and tryptophan. Crotonyl-CoA tetralithium is important in the metabolism of fatty acids and amino acids. Crotonyl-CoA tetralithium acts as a substrate for p300’s histone crotonyltransferase activity, competing with acetyl-CoA for p300-mediated histone acylation reactions. Crotonyl-CoA tetralithium 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 tetralithium 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 tetralithium can be used for the research of LPS-induced inflammatory response.
    Crotonyl-CoA tetralithium
  • HY-102060R
    WM-8014 (Standard)
    		Inhibitor
    WM-8014 (Standard) is the analytical standard of WM-8014 (HY-102060). This product is intended for research and analytical applications. WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.
    WM-8014 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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