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-N2020R
    Anacardic Acid (Standard)
    		Inhibitor
    Anacardic Acid (Standard) is the analytical standard of Anacardic Acid. This product is intended for research and analytical applications. 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.
    Anacardic Acid (Standard)
  • HY-177445
    KAT6-IN-4
    		Inhibitor
    KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER+/HER2- breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC).
    KAT6-IN-4
  • HY-103669
    HAT-IN-1
    		Inhibitor
    HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
    HAT-IN-1
  • HY-139149A
    (E/Z)-NiCur
    (E/Z)-NiCur is the active isomer of NiCur (HY-139149). (E/Z)-NiCur is a potent CBP histone acetyltransferase (HAT) inhibitor.
    (E/Z)-NiCur
  • HY-128362
    Ep300/CREBBP-IN-8
    		Inhibitor
    Ep300/CREBBP-IN-8 (Example 37) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.014 and 0.018 μM, respectively. Ep300/CREBBP-IN-8 can be used for the research of cancer.
    Ep300/CREBBP-IN-8
  • HY-159587
    P300-IN-4
    		Inhibitor
    P300-IN-4 (compound 6) is a (p300) inhibitor with the IC50 of 12.2 μM.
    P300-IN-4
  • HY-121009
    CCT077791
    		Inhibitor
    CCT077791 is a PCAF (IC50: 7.3 μM (FlashPlate); 2.2 μM (Filter assay)) and p300 histone acetyltransferase inhibitor. CCT077791 reduces total acetylation of histones H3 and H4, levels of specific acetylated lysine marks, and acetylation of α-tubulin. CCT077791 can be used in the research of colorectal cancer.
    CCT077791
  • HY-176251
    CBP/p300-IN-22
    		Inhibitor
    CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC50 of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.
    CBP/p300-IN-22
  • HY-RS07080
    KAT5 Human Pre-designed siRNA Set A
    		Inhibitor

    KAT5 Human Pre-designed siRNA Set A contains three designed siRNAs for KAT5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    KAT5 Human Pre-designed siRNA Set A
  • HY-146277
    CBP/p300-IN-19
    		Inhibitor
    CBP/p300-IN-19 is a potent 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 shows antitumor activity.
    CBP/p300-IN-19
  • HY-D2983
    ARHB
    ARHB is a highly selective and sensitive NAT2 fluorescent probe suitable for real-time detection of NAT2 activity in various bacteria. ARHB can successfully penetrate the bacterial cells, and the fluorescence intensity is positively correlated with the expression level of NAT2. ARHB is used for high-throughput screening of natural inhibitors for tuberculosis.
    ARHB
  • HY-161958
    dCE-2
    dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961)[1].
    dCE-2
  • HY-179657
    PROTAC MLT Degrader 1
    		Inhibitor
    PROTAC MLT Degrader 1 (M-PRORAC) is an asymmetric dual-functional degrader based on MLT PROTAC. PROTAC MLT Degrader 1 significantly reduces the protein level of p300 in the cell. PROTAC MLT Degrader 1 can be used in Alzheimer's disease research (pink: MLT ligand (HY-B0075); blue: CRBN ligand (HY-41547); black: linker (HY-140208)).
    PROTAC MLT Degrader 1
  • HY-134964R
    CTB (Standard)
    		Activator
    CTB (Standard) is the analytical standard of CTB. This product is intended for research and analytical applications. CTB is a potent p300 histone acetyltransferase activator. CTB can effectively induce apoptosis in MCF-7 cells.
    CTB (Standard)
  • HY-101027R
    GSK 4027 (Standard)
    		Inhibitor
    GSK 4027 (Standard) is the analytical standard of GSK 4027 (HY-101027). This product is intended for research and analytical applications. GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK 4027 (Standard)
  • HY-W614583
    4-Aminonaphthalen-1-yl acetate
    		Control
    4-Aminonaphthalen-1-yl acetate is a 4-amino-1-naphthol derivative and a negative control reagent for lysine (K) acetyltransferase KAT8. 4-Aminonaphthalen-1-yl acetate shows no activity against KAT8.
    4-Aminonaphthalen-1-yl acetate
  • HY-101084R
    NSC 228155 (Standard)
    		Inhibitor
    NSC 228155 (Standard) is the analytical standard of NSC 228155 (HY-101084). This product is intended for research and analytical applications. 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.
    NSC 228155 (Standard)
  • HY-100671R
    L002 (Standard)
    		Inhibitor
    L002 (Standard) is the analytical standard of L002 (HY-100671). This product is intended for research and analytical applications. L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.
    L002 (Standard)
  • HY-163824
    WIZ degrader 7
    		Degrader
    WIZ degrader 7 (Example 16) is a WIZ degrader with an IC50 value of < 0.01 μM. WIZ degrader 7 can be used to investigate sickle cell disease (SCD) and thalassemia.
    WIZ degrader 7
  • HY-W1122565
    KAT2A/B ligand 1
    		Ligand
    KAT2A/B ligand 1 (compound 32a) is a KAT2A/B ligand. KAT2A/B ligand 1 can be used as a target protein ligand for the synthesis of AUR1545 (HY-173158).
    KAT2A/B ligand 1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Acetyltransferase Isoform Comparison

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