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Histone Acetyltransferase inhibitors

Other Epigenetics Related Inhibitors

Histone Methyltransferase BET DNA Methyltransferase p300/CBP Histone Demethylase Histone 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
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.
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
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.
Transl Oncol, 2021, 14(11):101196
E1107 CTB CTB is a p300 activator and the lowest docked energy for this compound and p300 is 7.72 kcal/mol.
S7475 NU9056 NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. This compound demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells.

Signaling Pathway Map