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.
Histone Acetyltransferase Isoform Specific Products
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Histone Acetyltransferase Inhibitors
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Histone Acetyltransferase Agonist
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Histone Acetyltransferase Activators
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Histone Acetyltransferase Modulators
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Histone Acetyltransferase Degraders
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Histone Acetyltransferase Controls
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Histone Acetyltransferase Substrates
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Histone Acetyltransferase Ligands
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Histone Acetyltransferase Related Products (286)
Related Products (286)
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Antibodies (25)
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Histone Acetyltransferase Isoform Comparison
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Procyanidin B3
0 ImagesProcyanidin 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.
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(R,R)-dWIZ-1 TFA
0 ImagesCat. No.: HY-169761BPurity: 98.96%(R,R)-dWIZ-1 TFA is the (R,R) enantiomer of dWIZ-1 (HY-159098). dWIZ-1 is a potent WIZ molecular glue degrader. (R,R)-dWIZ-1 TFA can be used in studies related to sickle cell disease and β-thalassemia.
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CBPD-268
0 ImagesCBPD-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.
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Histone H4 (2-21)
0 ImagesHistone H4 (2-21) is a substrate peptide derived from the N-terminal region of histone H4, which serves as an acyl acceptor for lysine acetyltransferases of the MYST family (KAT). Histone H4 (2-21) participates in enzymatic reactions together with acyl-coenzyme A (acyl-CoA, and undergoes lysine acetylation and propionylation modifications catalyzed by KATs such as MOF. The apparent Km of Histone H4 (2-21) for MOF is 788.8 μM, while in the picNuA4 catalytic system, the Km and Kd values of the H4 peptide are 192 μM and 251 μM, respectively. Histone H4 (2-21) can be used in studies related to histone post-translational modifications, epigenetic regulation, and lysine acylation.
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L002
0 ImagesL002 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.
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TCIP3
0 ImagesSynonyms: KAT-TCIPTCIP3 is a bivalent molecular glue degrader that binds dually to p300/CBP and BCL6. TCIP3 redirects p300 and CBP, thereby activating programmed cell death genes that are normally repressed by the oncogenic driver gene BCL6. TCIP3 induces acetylation of BCL6 and histone tails, inhibits c-MYC transcription. TCIP3 can be used for the research of diffuse large B-cell lymphoma (DLBCL).
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PCAF-IN-1
0 ImagesPCAF-IN-1 is a highly selective PCAF inhibitor. PCAF-IN-1 is a antitumor agents, which can be used in tumor research research.
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GSK699
0 ImagesGSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases.
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Histone Acetyltransferase Inhibitor II
0 ImagesHistone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
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GSK4028
0 ImagesGSK4028 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.
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Ifupinostat
0 ImagesSynonyms: BEBT-908Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research.
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DS-9300
0 ImagesDS-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.
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KI-TOX-A3
0 ImagesKI-TOX-A3 is a TOX protein-protein interaction inhibitor that blocks the TOX-KAT7 protein-protein interaction with an IC50 of 0.51 μM. KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses exhaustion of CD8+ T cells, and inhibits the proliferation of T cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 shows promise for use in studies of hematological malignancies such as T-ALL.
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PH14
0 ImagesPH14 is a PI3Kα/HDAC3 inhibitor, with an IC50 value of 20.3 nM against PI3Kα and 24.5 nM against HDAC3. PH14 blocks the phosphorylation of AKT, inhibits the PI3K/AKT signaling pathway, increases the level of acetylated histone H3, promotes apoptosis, and exerts antiproliferative activity against tumor cells. PH14 can be used in the research of mantle cell lymphoma, myeloma, acute promyelocytic leukemia, and breast cancer.
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Curcumin-d6
0 ImagesSynonyms: Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). 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 is a photosensitizer against microorganisms. 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.
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YF-2 hydrochloride
0 ImagesYF-2 hydrochloride 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.
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XX-650-23
0 ImagesXX-650-23 is a potent CREB inhibitor. XX-650-23inhibits CREB function through disruption of CBP-CREB interaction. XX-650-23 can be used for AML research.
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Ac-Lys(CoA)-NH2 TFA
0 ImagesSynonyms: Ac-Lys(coenzyme A)-NH2 TFALys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.
