1. Signaling Pathways
  2. Epigenetics
  3. Histone Acetyltransferase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-66005S2
    Acetaminophen-d7
    ≥99.0%
    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.
    Acetaminophen-d<sub>7</sub>
  • HY-101027A
    GSK4028
    98.06%
    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
  • HY-110263
    EML 425
    Inhibitor 98.16%
    EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
    EML 425
  • HY-152241
    DS-9300
    Inhibitor 99.83%
    DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.
    DS-9300
  • HY-153768
    KAT modulator-1
    Modulator ≥98.0%
    KAT modulator-1 (Compound 3) is a KAT modulator. KAT modulator-1 can interact with p300 full-length but not with the catalytic domain. KAT modulator-1 can be used for epigenetics research.
    KAT modulator-1
  • HY-149470
    MOZ-IN-3
    Inhibitor 98.75%
    MOZ-IN-3 (Compound 6j) is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). MOZ-IN-3 has antitumor activity against four different myeloid leukemia cell lines (HL-60, U937, SKNO-1, K562). MOZ-IN-3 has favorable metabolic stability and pharmacokinetics.
    MOZ-IN-3
  • HY-161369
    CBPD-268
    Degrader
    CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker).
    CBPD-268
  • HY-120290
    PU141
    Inhibitor 99.30%
    PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
    PU141
  • HY-139108
    DCH36_06
    Inhibitor 99.19%
    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.
    DCH36_06
  • 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.
    MOZ-IN-2
  • HY-139149
    NiCur
    Inhibitor 99.11%
    NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC50 value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.
    NiCur
  • HY-115539
    Windorphen
    Inhibitor 99.75%
    Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP.
    Windorphen
  • HY-104068
    Naphthol AS-E
    Inhibitor ≥98.0%
    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
  • HY-111954
    (+)-Erinacin A
    99.97%
    (+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage.
    (+)-Erinacin A
  • HY-66005R
    Acetaminophen (Standard)
    99.94%
    Acetaminophen (Standard) is the analytical standard of Acetaminophen. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0005S
    Curcumin-d6
    Inhibitor 98.00%
    Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
    Curcumin-d<sub>6</sub>
  • HY-146277A
    CBP/p300-IN-19 hydrochloride
    Inhibitor
    CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity.
    CBP/p300-IN-19 hydrochloride
  • HY-149306
    MS78
    99.38%
    MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker.
    MS78
  • HY-100132
    CBP/p300-IN-5
    Inhibitor
    P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM.
    CBP/p300-IN-5
  • HY-151812
    CBP/p300-IN-20
    Inhibitor 98.03%
    CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.
    CBP/p300-IN-20
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