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-120317
    CPTH2-Alkyne
    		Inhibitor ≥99.0%
    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-145954
    NAT2-IN-1
    		Inhibitor 99.0%
    NAT2-IN-1 (APA) is an inhibitor of agent metabolic enzyme N-acetyltransferase 2 (NAT2). NAT2-IN-1 can selectively kill slow NAT2 cells.
    NAT2-IN-1
  • HY-163820
    WIZ degrader 4
    		Degrader 99.37%
    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-134621
    P300-IN-1
    		Inhibitor
    P300-IN-1 (cpd205) is a Histone acetylase p300 inhibitor.
    P300-IN-1
  • HY-W013274A
    CPTH2 hydrochloride
    		Inhibitor
    CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
    CPTH2 hydrochloride
  • HY-162259
    QC-182
    		Degrader
    QC-182 is a potent PROTAC degrader of p300/CBP. QC-182 reduces p300 protein in the SK-HEP-1 cells (DC50 = 93nM). QC-182 potently and effectively inhibits cell growth in the SK-HEP-1 and JHH7 cell lines with IC50 values of 0.733 and 0.477 μM, respectively. QC-182 can be used for the research of hepatocellular carcinoma (HCC).
    QC-182
  • HY-143443
    DS17701585
    		Inhibitor
    DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research.
    DS17701585
  • HY-141546
    Pocenbrodib
    		Inhibitor
    Pocenbrodib (compound II) is a CBP/p300 family of bromodomain inhibitor. Pocenbrodib has the potential for cancer research.
    Pocenbrodib
  • HY-P2557
    Histone H3 (5-23)
    Histone H3 (5-23), derived from histone H3 5-23 amino acids, can be used as a substrate for histone acetyltransferase (HAT) assays.
    Histone H3 (5-23)
  • HY-P2515
    Transcriptional Intermediary Factor 2 (TIF2) (740-753)
    		Agonist
    Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a TIF-2 coactivator peptide composed of 14 amino acids and covers the residue range 740-753 of TIF-2 protein.
    Transcriptional Intermediary Factor 2 (TIF2) (740-753)
  • 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).
    CBP/p300-IN-14
  • 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.
    CBP/p300-IN-18
  • 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.
    Ep300/CREBBP-IN-4
  • 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.
    CBP/p300-IN-21
  • HY-143339
    CBP/p300-IN-15
    		Inhibitor
    CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC50 values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC50 values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research.
    CBP/p300-IN-15
  • HY-177044
    KAT6A/KAT7-IN-2
    		Inhibitor
    KAT6A/KAT7-IN-2 (Example 177) is a KAT6A and KAT7 inhibitor. KAT6A/KAT7-IN-2 has IC50 values of both ≤ 1 nM for KAT6A and KAT7. KAT6A/KAT7-IN-2 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-2 also inhibits tumor cell proliferation, with an IC50 of ≤ 100 nM for CAMA-1. KAT6A/KAT7-IN-2 can be used in the study of cancer.
    KAT6A/KAT7-IN-2
  • HY-128364
    Ep300/CREBBP-IN-3
    		Inhibitor
    Ep300/CREBBP-IN-3 (Example 61) is a potent Ep300 and CREBBP inhibitor with IC50s of 0.056 and 0.095 μM, respectively. Ep300/CREBBP-IN-3 can be used for the research of cancer.
    Ep300/CREBBP-IN-3
  • HY-146445
    P300 bromodomain-IN-1
    		Inhibitor
    P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells.
    P300 bromodomain-IN-1
  • HY-177043
    KAT6A/KAT7-IN-1
    		Inhibitor
    KAT6A/KAT7-IN-1 (Example 113) is a KAT6A and KAT7 inhibitor. The IC50 of KAT6A/KAT7-IN-1 for KAT6A is > 1 nM but ≤ 10 nM, while the IC50 for KAT7 is ≤ 1 nM. KAT6A/KAT7-IN-1 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-1 also inhibits tumor cell proliferation, with an IC50 of > 2 μM but ≤ 5 μM for CAMA-1. KAT6A/KAT7-IN-1 can be used in the study of cancer.
    KAT6A/KAT7-IN-1
  • HY-143440
    CBP/p300-IN-16
    		Inhibitor
    CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC50s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively.
    CBP/p300-IN-16
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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