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 (285)
Related Products (285)
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Antibodies (25)
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Histone Acetyltransferase Isoform Comparison
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PROTAC p300 degrader-1
0 ImagesCat. No.: HY-183251PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL).
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ROCK2-IN-13
0 ImagesCat. No.: HY-179498ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach.
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GSK702
0 ImagesCat. No.: HY-185009CAS No.: 2260944-69-0GSK702, a PROTAC, is a the less active cis-(S,S)-enantiomer of GSK983 (P300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) PROTAC). GSK702 induces only a small decrease of PCAF protein levels. GSK702 binds to CRBN and causes a reduction of IL-1β in macrophages. GSK702 can be used for the study of inflammatory mediators.
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4-Pentynoyl-Coenzyme A TFA
0 ImagesCat. No.: HY-CE00983ASynonyms: 4-Pentynoyl-CoA TFA4-Pentynoyl-Coenzyme A (4-Pentynoyl-CoA) TFA is an analog of the natural substrate acetyl-CoA (Acetyl-CoA) (HY-114293). 4-Pentynoyl-Coenzyme A TFA can replace acetyl-CoA to be recognized and utilized by lysine acetyltransferases such as p300. 4-Pentynoyl-Coenzyme A TFA can be conjugated to azide probes carrying fluorescent groups (e.g., Rhodamine-azide) or biotin (Biotin-azide) via Cu (I)-catalyzed azide-alkyne cycloaddition (CuAAC).
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BAY-7728
0 ImagesBAY-7728 is an orally active and selective dual inhibitor of KAT6A (IC50: 45 nM)/KAT6B (IC50: 95 nM). BAY-7728 can effectively inhibit tumor growth and regulate the acetylation level of histone H3K23. BAY-7728 can be used for tumor research.
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NSC 698600
0 ImagesCat. No.: HY-147289CAS No.: 908069-17-0NSC 698600 is a potent PCAF inhibitor, with IC50 of 6.51 µM (PCAF/H31-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells.
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KAT2A degrader-1
0 ImagesCat. No.: HY-187168CAS No.: 2407654-72-0KAT2A degrader-1 is a molecular glue degrader targeting KAT2A, with a DC50 of 89 nM in Kelly cells. KAT2A degrader-1 recruits KAT2A to cereblon (CRBN) in a degron-independent manner, forms a ternary complex with KAT2A and CRBN, and drives the polyubiquitination and proteasome-dependent degradation of KAT2A. KAT2A degrader-1 reduces the level of histone H3 lysine 9 acetylation (H3K9Ac). KAT2A degrader-1 induces antiproliferative effects in acute myeloid leukemia cells, while enhancing KAT2A-CRBN dimerization activity and eliminating the targeting effect on GSPT1. KAT2A degrader-1 can be used for research related to acute myeloid leukemia.
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Acetaminophen-13C6
0 ImagesCat. No.: HY-66005S3CAS No.: 2132405-57-1Synonyms: Paracetamol-13C6; 4-Acetamidophenol-13C6; 4'-Hydroxyacetanilide-13C6Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-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.
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SL010110
0 ImagesCat. No.: HY-W197205CAS No.: 380173-90-0SL010110 is an anti-hyperglycemic agent. SL010110 potently inhibits gluconeogenesis by inhibiting SIRT2, activating p300, and subsequently promoting PEPCK1 degradation. SL010110 downregulates the protein level of PEPCK1 without affecting the gene expressions of PEPCK, glucose-6-phosphatase, and fructose-1,6-bisphosphatase. SL010110 significantly improves glucose homeostasis in type 2 diabetic (T2D) mice model. SL010110 can be used for T2D research.
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DC-CPin7
0 ImagesCat. No.: HY-147869CAS No.: 893781-17-4DC-CPin7 is a potent inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 2.5 μM.
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P300-IN-6
0 ImagesCat. No.: HY-181669CAS No.: 3034595-62-2P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma.
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EP300/CBP ligand 3
0 ImagesCat. No.: HY-184454CBP/p300 ligand 11 is a ligand of EP300 and CBP, which can be used for PROTAC synthesis, such as serving as the target protein ligand of PROTAC CBP/EP300 Degrader-5 (HY-184453).
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iP300w
0 ImagesCat. No.: HY-174868CAS No.: 3055107-60-0iP300w (Compound 9) is a Histone acetyltransferase p300 (KAT3B) inhibitor. iP300w can be used for synthesis of PROTAC BT-O2C (HY-174866).
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Y16526
0 ImagesCat. No.: HY-168464Y16526 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.03 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).
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PROTAC CBP/EP300 degrader-1
0 ImagesCat. No.: HY-184453PROTAC CBP/EP300 Degrader-5 is a CBP and EP300 PROTAC degrader. PROTAC CBP/EP300 Degrader-5 relies on the ubiquitin-proteasome pathway to preferentially induce ubiquitination and degradation of EP300 rather than CBP. PROTAC CBP/EP300 Degrader-5 induces G1 phase cell cycle arrest and triggers Apoptosis. PROTAC CBP/EP300 Degrader-5 is applicable to research related to EP300-dependent malignant tumors.
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XYD198
0 ImagesCat. No.: HY-161498XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia.
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dCBP-30
0 ImagesCat. No.: HY-184556dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC50 values of 0.05 nM (CBP) and 0.04 nM (p300), respectively. dCBP-30 reduces the acetylation levels of histone substrates H3K27, H3K18, H2BK5 and H2BK20, downregulates multiple myeloma-specific dependency programs, and induces multiple myeloma cell apoptosis. dCBP-30 triggers tumor regression and prolongs survival in multiple myeloma xenograft mouse models, and exhibits synergistic antiproliferative activity with dexamethasone. dCBP-30 can be used for the research of multiple myeloma.
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KAT6A-IN-2
0 ImagesCat. No.: HY-162995CAS No.: 2991087-74-0KAT6A-IN-2 (compund 7) is a KAT6A inhibitor.
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SYY-B085-1
0 ImagesCat. No.: HY-138945CAS No.: 2379416-47-2SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor extracted from patent WO2019201291A1.
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XYD129
0 ImagesCat. No.: HY-161710XYD129 is a CBP/p300 PROTAC degrader. XYD129 potently binds to CBP, p300 and CRBN proteins, with IC50 values of 0.021 μM, 0.03 μM and 0.18 μM, respectively. XYD129 forms a ternary CRBN-CBP/p300 complex and induces CBP/p300 degradation via the ubiquitin-proteasome system. XYD129 inhibits tumor growth and suppresses the proliferation of acute myeloid leukemia cells. XYD129 can be used in studies related to acute myeloid leukemia.
