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-161483
    CBP/p300 ligand 3
    		Inhibitor
    CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function.
    CBP/p300 ligand 3
  • HY-120317
    CPTH2-Alkyne
    		Inhibitor
    CPTH2-Alkyne is a cell active analog of CPTH2 (HY-W013274). CPTH2-Alkyne specifically accumulates in nucleoli and locates in nuclear periphery and in cytoplasma. CPTH2-Alkyne inhibits N-acetyltransferase 10 (NAT10). CPTH2-Alkyne is used in study of nuclear architecture and application in laminopathy.
    CPTH2-Alkyne
  • HY-125969
    Rtt109 inhibitor 1
    		Inhibitor
    Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site.
    Rtt109 inhibitor 1
  • HY-161958
    dCE-2
    dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961)[1].
    dCE-2
  • HY-124892A
    Acetylethylcholine mustard hydrochloride
    		Inhibitor
    Acetylethylcholine mustard hydrochloride (Acetyl-AF64) is an inhibitor of choline acetyl-transferase that reduces the contraction frequency of the myotubes by inhibiting the synthesis of acetylethylcholine (Ach) with the half-maximal inhibitory concentration (IC50) of 1.22 mM. Acetylethylcholine mustard hydrochloride is an irreversible ligand for the high affinity choline transport system. Acetylethylcholine mustard hydrochloride is also a cholinotoxin. Acetylethylcholine mustard hydrochloride is a precursor for ethylcholine mustard aziridinium ion.
    Acetylethylcholine mustard hydrochloride
  • HY-139804
    CTK7A
    		Inhibitor
    CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer treatment research.
    CTK7A
  • HY-163824
    WIZ degrader 7
    		Degrader
    WIZ degrader 7 (Example 16) is a WIZ degrader with an IC50 value of < 0.01 μM. WIZ degrader 7 can be used to investigate sickle cell disease (SCD) and thalassemia.
    WIZ degrader 7
  • HY-163820
    WIZ degrader 4
    		Degrader
    WIZ degrader 4 (Example 1) is a WIZ degrader with an AC50 value of 160 nM. WIZ degrader 4 can be used to investigate sickle cell disease (SCD) and thalassemia.
    WIZ degrader 4
  • 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-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-N0005S1
    Curcumin-d3
    		Inhibitor
    Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin. 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 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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