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-123604
    TH1834
    		Inhibitor 99.79%
    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.
    TH1834
  • HY-158009
    SGF29-IN-1
    		Inhibitor 98.0%
    SGF29-IN-1 (Compound Cpd_DC60) is a selective inhibitor for Spt-Ada-Gcn5 acetyltransferase (SAGA)–associated factor 29 (SGF29)-Tudor domain. SGF29-IN-1 exhibits activity against leukemia.
    SGF29-IN-1
  • HY-149302
    MC4033
    		Inhibitor 98.26%
    MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively.
    MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells.
    MC4033
  • HY-159099
    WIZ degrader 9
    		Degrader 99.29%
    WIZ degrader 9 is an orally active molecular glue degrader of the WIZ transcription factor. As a molecular glue, WIZ degrader 9 recruits WIZ to the cereblon E3 ubiquitin ligase complex via its ZF7 domain, driving proteasome-dependent degradation of WIZ. WIZ degrader 9 induces hemoglobin production, reduces the level of H3K9 dimethylation across the whole genome and at the β-globin locus, upregulates the transcription of γ-globin and BGLT3, and increases the level of histone H3K9 acetylation in the promoter region of HBG1/2. WIZ degrader 9 effectively induces fetal hemoglobin production in both mice and cynomolgus monkeys. WIZ degrader 9 can be used for research on sickle cell disease.
    WIZ degrader 9
  • HY-173158
    AUR1545
    		Inhibitor 99.58%
    AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid leukemia cells. AUR1545 inhibits cell growth, induces epithelial differentiation and suppresses tumor growth in small cell lung cancer models. AUR1545 inhibits cell growth and induces differentiation in neuroendocrine prostate cancer cells and primary patient-derived organoids. AUR1545 is applicable to research related to acute myeloid leukemia, small cell lung cancer and neuroendocrine prostate cancer.
    AUR1545
  • HY-66005S
    Acetaminophen-d4
    		99.60%
    Acetaminophen-d4 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>4</sub>
  • HY-19541
    I-CBP112
    		Activator 98.43%
    I-CBP112, a chemical probe, is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
    I-CBP112
  • HY-153604
    MC4171
    		Inhibitor 99.37%
    MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer.
    MC4171
  • HY-175742
    BMS-986470
    		Degrader 99.78%
    BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ. BMS-986470 has potent γ-globin induction activity. BMS-986470 can be used for sickle cell disease (SCD) research.
    BMS-986470
  • HY-120028
    GNE-207
    		Inhibitor 99.94%
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
    GNE-207
  • HY-16531
    YF-2
    		Activator 98.76%
    YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
    YF-2
  • HY-141894
    5-Ph-IAA-AM
    		Activator 99.04%
    5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA (HY-134653) analog which contains an acetoxymethyl (AM) group. 5-Ph-IAA-AM affords an enhanced protein degradation in laid embryos. 5-Ph-IAA-AM can be used to disclosure the roles of proteins in C. elegans, in particular those that are involved in embryogenesis and development, through temporally controlled protein degradation.
    5-Ph-IAA-AM
  • HY-156140
    Naa50-IN-1
    		Inhibitor 99.94%
    Naa50-IN-1 is an N-alpha-acetyltransferase 50 (Naa50) inhibitor with an IC50 of 7 nM against the human protein. Naa50-IN-1 exhibits selectivity toward the related enzymes Naa10 and Naa60. Naa50-IN-1 binds to the substrate-binding pocket of Naa50, and its binding affinity is enhanced by AcCoA.
    Naa50-IN-1
  • HY-66005R
    Acetaminophen (Standard)
    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-N2345
    Procyanidin B3
    		Inhibitor 99.92%
    Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
    Procyanidin B3
  • HY-123604A
    TH1834 dihydrochloride
    		Inhibitor 99.89%
    TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
    TH1834 dihydrochloride
  • HY-169761B
    (R,R)-dWIZ-1 TFA
    		Control 98.58%
    (R,R)-dWIZ-1 TFA is the the (R,R)-enantiomer of dWIZ-1 (HY-159098). dWIZ-1 is a potent WIZ molecular glue degrader. dWIZ-1 has the potential for the research of sickle cell disease (SCD).
    (R,R)-dWIZ-1 TFA
  • 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.
    BAY-184
  • HY-154984
    JET-209
    		Degrader 98.07%
    JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia.
    JET-209
  • HY-161369
    CBPD-268
    		Degrader 99.23%
    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 (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker).
    CBPD-268
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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