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PRMT Inhibitors

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

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
E1349 TNG908 (Ralometostat) Ralometostat (TNG908) is a potent, selective, and brain-penetrant inhibitor of PRMT5 with an IC50 of 4 μM, acting through an MTA-cooperative mechanism. It also shows antitumor activity in a xenograft model.
S8664 GSK3326595 (Pemrametostat, EPZ015938) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
MedComm (2020), 2025, 6(6):e70150
J Med Chem, 2025, 68(4):4217-4236
J Med Chem, 2025, 68(5):5097-5119
S8883 LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. It shows antitumor activity.
Nucleic Acids Research, 2026, gkag016
Mol Cancer Res, 2025, 23(2):107-118
Res Sq, 2025, rs.3.rs-5936706
S8112 MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
Biol Direct, 2025, 20(1):60
Hepatol Commun, 2025, 9(4)e0647
J Immunother Cancer, 2024, 12(9)e009603
S6737 C7280948 C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.
Cell Death Differ, 2025, 10.1038/s41418-025-01585-6
Cell Death Dis, 2023, 14(4):233
Cell Death Dis, 2023, 14(8):512
S8858 GSK3368715 3HCl GSK3368715 3HCl is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
Nat Commun, 2023, 14(1):2806
Mol Cell, 2023, 83(15):2810-2828.e6
JCI Insight, 2022, 7(10)e151353
E1024 MRTX1719 (Navlimetostat) MRTX1719 is a potent, selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5•MTA), a potentially tumor-selective target for therapeutic intervention.
Bioconjugate Chemistry, 2025, nan
bioRxiv, 2025, 2025.07.11.664387
Anticancer Research, 2024, 5231-5240
S0855 TC-E 5003 TC-E 5003 (NSC 30176, Compound 2e) is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with IC50 of 1.5 μM. This compound modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.
Biol Direct, 2025, 20(1):60
Hepatol Commun, 2025, 9(4)e0647
Mol Ther, 2023, 10.1016/j.ymthe.2023.09.011
E1088 TP-064

TP-064 is a potent and selective small molecule inhibitor of PRMT4 with IC50 < 10 nM, >100 fold more selective for PRMT4 than other PRMTs.
Cell Rep Med, 2023, 4(12):101326
E1007 BRD0639

BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilized and living cells, respectively.