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.
Histone Acetyltransferase Isoform Specific Products
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Histone Acetyltransferase Inhibitors
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Histone Acetyltransferase Agonist
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Histone Acetyltransferase Activators
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Histone Acetyltransferase Modulators
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Histone Acetyltransferase Degraders
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Histone Acetyltransferase Controls
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Histone Acetyltransferase Substrates
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Histone Acetyltransferase Ligands
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Histone Acetyltransferase Related Products (288)
Related Products (288)
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Antibodies (25)
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Histone Acetyltransferase Isoform Comparison
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Acetaminophen-d5
0 ImagesCat. No.: HY-66005S5Synonyms: Paracetamol-d5; 4-Acetamidophenol-d5; 4'-Hydroxyacetanilide-d5Acetaminophen-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.
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CPI-637 (Standard)
0 ImagesCat. No.: HY-100482RCAS No.: 1884712-47-3CPI-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.
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GSK4028 (Standard)
0 ImagesCat. No.: HY-101027ARCAS No.: 2079886-19-2GSK4028 (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.
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I-CBP112 hydrochloride
0 ImagesCat. No.: HY-19541ACAS No.: 2147701-33-3I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
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SGC-CBP30 (Standard)
0 ImagesCat. No.: HY-15826RCAS No.: 1613695-14-9SGC-CBP30 (Standard) is the analytical standard of SGC-CBP30 (HY-15826). This product is intended for research and analytical applications. SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
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Naphthol AS-E (Standard)
0 ImagesCat. No.: HY-104068RCAS No.: 92-78-4Naphthol 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.
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WIZ degrader 6
0 ImagesCat. No.: HY-163823CAS No.: 3036553-87-1WIZ degrader 6 (compound 10) is a WIZ molecular glue degrader with the EC50 of <0.01 μM. WIZ degrader 6 can be used for study of sickle cell disease.
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WIZ degrader 5
0 ImagesCat. No.: HY-163822CAS No.: 2879250-73-2WIZ degrader 5 (example 41) is a molecular glue degrader for widely interspaced zinc (WIZ) finger motifs with an AC50 of 0.14 nM. WIZ degrader 5 induces the expression of fetal hemoglobin (HbF) with an EC50 of 25 nM. WIZ degrader 5 can be used in research related to hereditary blood disorders, such as sickle cell disease (SCD) and thalassemia.
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GNE-781 (Standard)
0 ImagesCat. No.: HY-108696RCAS No.: 1936422-33-1GNE-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.
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Curcumin-d3
0 ImagesCat. No.: HY-N0005S1Synonyms: Diferuloylmethane-d3; Natural Yellow 3-d3; Turmeric yellow-d3Curcumin-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.
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GNE-049 (Standard)
0 ImagesCat. No.: HY-108435RCAS No.: 1936421-41-8GNE-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.
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WM-3835 (Standard)
0 ImagesCat. No.: HY-134901RCAS No.: 2229025-70-9WM-3835 (Standard) is the analytical standard of WM-3835 (HY-134901). This product is intended for research and analytical applications. WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
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EML 425 (Standard)
0 ImagesCat. No.: HY-110263RCAS No.: 1675821-32-5
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Crotonyl-CoA
0 ImagesCrotonyl-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.
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Garcinol (Standard)
0 ImagesCat. No.: HY-107569RCAS No.: 78824-30-3Garcinol (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.
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GNE-272 (Standard)
0 ImagesCat. No.: HY-100726RCAS No.: 1936428-93-1GNE-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.
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NU9056 (Standard)
0 ImagesCat. No.: HY-110127RCAS No.: 1450644-28-6NU9056 (Standard) is the analytical standard of NU9056 (HY-110127). This product is intended for research and analytical applications. NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 μM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells.
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3,5-DMA hydrochloride
0 ImagesCat. No.: HY-W713313CAS No.: 24973-29-3Synonyms: 3,5-Dimethoxyamphetamine hydrochloride3,5-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.
