SETD

Other Methylation Related Inhibitors

EZH2 PRMT MAT2A LSD1 JMJD G9a/GLP MLL COMT DOT1 HNMT

Cat.No.	Product Name	Information	Product Use Citations
E1179	EZM0414	EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2.	Journal of Orthopaedic Translation, March 28, 2024, 211-225 Cancer Research, March 02, 2026, 1180-1193
S7570	UNC0379	UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases.	Mol Cancer, 2025, 24(1):102 Cell Death Dis, 2025, 16(1):226 Res Sq, 2024, rs.3.rs-4603170
S7294	PFI-2 HCl	PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with K_{i (app)} and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.	Life Science Alliance, March 21, 2023, e202201619 Pharmacological Research, March 2022, 106122 bioRxiv, January 16, 2026, 2026.01.15.699551
S7983	A-196	A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.	Molecular Cancer Therapeutics, 2025, 1020-1029 Gene & Protein in Disease, 2025, 8441 iScience, 2023, 26(3):106158
S4635	Cyproheptadine hydrochloride sesquihydrate	Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.	Frontiers in Pharmacology, 2025, 1539032 World Journal of Gastroenterology, 2023, 3103-3118 Anticancer Res, 2019, 39(7):3767-3775