1. Signaling Pathways
  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 (51):

Cat. No. Product Name Effect Purity
  • HY-107455
    A-485
    Inhibitor ≥98.0%
    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.
  • HY-N0005
    Curcumin
    Inhibitor
    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-66005
    Acetaminophen
    99.96%
    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-13823
    C646
    Inhibitor ≥98.0%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
  • HY-N2020
    Anacardic Acid
    Inhibitor ≥98.0%
    Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.
  • HY-132283
    PF-9363
    Inhibitor 99.53%
    PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.
  • HY-139108
    DCH36_06
    Inhibitor 99.22%
    DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
  • HY-132197
    CBP/p300-IN-12
    Inhibitor
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
  • HY-102058
    WM-1119
    Inhibitor ≥98.0%
    WM-1119 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.
  • HY-15887
    MG 149
    Inhibitor 99.07%
    MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM).
  • 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.
  • HY-16706A
    Remodelin hydrobromide
    Inhibitor 99.49%
    Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity.
  • HY-108696
    GNE-781
    Inhibitor 98.19%
    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.
  • HY-101084
    NSC 228155
    Inhibitor ≥98.0%
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
  • HY-107569
    Garcinol
    Inhibitor ≥98.0%
    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.
  • HY-100482
    CPI-637
    Inhibitor 99.94%
    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.
  • HY-108435
    GNE-049
    Inhibitor 98.98%
    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.
  • HY-100726
    GNE-272
    99.74%
    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.
  • HY-136938
    NEO2734
    Inhibitor 99.79%
    NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains. NEO2734 is active in SPOP mutant and wild-type prostate cancer.
  • HY-102060
    WM-8014
    Inhibitor 99.64%
    WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.
Isoform Specific Products

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