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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.
Cancer Discovery, September 19, 2025, 155-176
Nutrients, November 24, 2025, 3673
Proceedings of the National Academy of Sciences, December 24, 2025, e2516667122
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
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
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
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.
ImmunoTargets and Therapy, 2025, 1145-1158
Cancer Discovery, 2022, 1804-1823
Cancer Discov, 2022, candisc.0646.2021
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.
Nature Genetics, 2025, nan
Nat Genet, 2025, 57(10):2468-2481
Nature Genetics, 2025, 2468-2481
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
S1242 CPTH2 CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. This compound induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B.
PLOS ONE, 2024, e0299145
Transl Oncol, 2021, 14(11):101196
Translational Oncology, 2021, 101196

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