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Histone Acetyltransferase inhibitors

Other Epigenetics Related Inhibitors

Histone Methyltransferase BET DNA Methyltransferase p300/CBP Histone Demethylase MicroRNA NSD EZH1 RNA Methyltransferase SF3B

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
E0146 PF-9363 (CTx-648) PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumor activity in ER+ breast cancer models.
S8740 A-485 A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.
Nat Genet, 2025, 57(10):2468-2481
Cancer Discov, 2025, 15(2):382-400
Nat Cell Biol, 2025, 10.1038/s41556-025-01658-1
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Nat Commun, 2025, 16(1):4502
Nat Commun, 2025, 16(1):524
J Extracell Vesicles, 2025, 14(2):e70042
Verified customer review of C646
S7641 Remodelin Hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
Genome Med, 2025, 17(1):90
Int J Biol Sci, 2025, 21(11):4997-5014
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
S7476 MG149 MG149 (Tip60 HAT inhibitor) is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF, respectively.
Redox Biol, 2025, 85:103722
Cells, 2025, 14(14)1100
Int J Mol Sci, 2024, 25(17)9600
S8776 WM-1119 WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively.
Cancer Discov, 2022, candisc.0646.2021
Theranostics, 2021, 11(13):6278-6292
Biochem Biophys Res Commun, 2021, 585:185-190
S0022 YF-2 YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, this compound has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. It also increases p300 activity.
J Extracell Vesicles, 2025, 14(2):e70042
J Exp Clin Cancer Res, 2022, 41(1):77
E1215 JQAD1 JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation.
Nat Genet, 2025, 57(10):2468-2481
bioRxiv, 2024, 2024.03.29.587346
S2977 EML 425 EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
Cell Death Dis, 2024, 15(10):755
bioRxiv, 2024, 2024.02.22.581432
S9805 WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
Cell Mol Life Sci, 2025, 82(1):140
Cell Oncol (Dordr), 2025, 48(4):943-959

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