2. Epigenetics
  3. Histone Acetyltransferase

Histone Acetyltransferase

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 Related Products (140):

Cat. No. Product Name Effect Purity
  • HY-134901
    WM-3835 Inhibitor 99.78%
    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[1].
  • HY-13823
    C646 Inhibitor 99.78%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases[1].
  • HY-66005
    Acetaminophen 99.98%
    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 induces ferroptosis and leads to acute liver injury in mice model[5].
  • HY-107455
    A-485 Inhibitor
    A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively[1].
  • HY-N0005
    Curcumin Inhibitor 98.84%
    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.
  • HY-159957
    BAY-184 Inhibitor 99.00%
    BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth[1].
  • 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[1].
  • HY-159587
    P300-IN-4 Inhibitor
    P300-IN-4 (compound 6) is a (p300) inhibitor with the IC50 of 12.2 μM.
  • 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)[1].
  • HY-15826
    SGC-CBP30 Inhibitor 99.83%
    SGC-CBP30 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[1][2][3].
  • HY-139861
    CBP/p300-IN-14 Inhibitor
    CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC50 of 3.3 nM (extracted from patent WO2021213521A1, compound 27)[1].
  • HY-143442
    CBP/p300-IN-18 Inhibitor
    CBP/p300-IN-18 (compound 8) is a potent EP300/CBP HAT inhibitor with IC50s of 0.056, 0.46 µM for HAT EP300 and LK2 H3K27, respectively[1].
  • HY-102059
    MOZ-IN-2 Inhibitor 99.87%
    MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC50 of 125 μM.
  • HY-128367
    Ep300/CREBBP-IN-4 Inhibitor
    Ep300/CREBBP-IN-4 (Example 56) is a potent Ep300 and CREBBP inhibitor with IC50s of 0.024 and 0.064 μM, respectively. Ep300/CREBBP-IN-4 can be used for the research of cancer[1].
  • HY-123604
    TH1834 Inhibitor 99.60%
    TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity[1].
  • HY-141546
    Pocenbrodib Inhibitor
    Pocenbrodib (compound II) is a CBP/p300 family of bromodomain inhibitor. Pocenbrodib has the potential for cancer research[1].
  • HY-155229
    CBP/p300-IN-21 Inhibitor
    CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC50: 0.07 and 1.755 μM for p300 and CBP). CBP/p300-IN-21 decreases H3K18Ac level. CBP/p300-IN-21 inhibits growth of 4T1 tumor growth in mice[1].
  • 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[1]. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation[2]. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment[3].
  • HY-66005S2
    Acetaminophen-d7
    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.
  • HY-134964
    CTB Activator 99.93%
    CTB is a potent p300 histone acetyltransferase activator[1]. CTB can effectively induce apoptosis in MCF-7 cells[2].