Home Methylation PRMT

PRMT Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S8479 LLY-284 LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. This compound is much less active than LLY-283 and can be used as a negative control for it.
E1871New TNG-462 TNG-462 is an orally active, potent and selective inhibitor of methylthioadenosine (MTA)-cooperative PRMT5. It exhibits significant antitumor activity, including durable regressions and complete responses, against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation solid tumors.
E1600 AMG 193 AMG-193 is an orally active and MTA-cooperative inhibitor of PRMT5 with potent biochemical and cellular activity. AMG-193, in combination with MTA, selectively targets and inhibits the growth of MTAP-deficient tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor activity.
E2887 MS023 hydrochloride MS023 hydrochloride(Compound 3) is a potent, selective and cell-active inhibitor of human type I protein arginine methyltransferases (PRMT), with IC50 values of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
E1481New AM-9747 AM-9747 (PRMT5-IN-25) is a potent inhibitor of PRMT5 with a Ki of 0.06 nM. It exhibits antiproliferative activity and a significant oral antitumor effect in mouse models employing patient-derived xenografts (PDX).
S0184 XY1 XY1 is an inactive, close analog of SGC707 that can be used as the negative control for SGC707. SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
E4612 iCARM1 iCARM1 (CARM1-IN-6) is a potent and selective inhibitor of protein arginine methyltransferase CARM1 (PRMT4) with an IC50 of 12.3 μM. It potently suppresses breast cancer cell growth both in vitro and in vivo and can be used in cancer research.
E4701 CMP-5 CMP5 is a potent and selective small molecule inhibitor of PRMT5. It is found to selectively block S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. It also exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes.
E1658 PRT543 PRT543 is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad antitumor activity in vitro and in vivo. It also inhibits the methyltransferase activity of the PRMT5/MEP50 complex with an IC50 of 10.8 nM.
E1429 T1-44 T1-44 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits anti-tumor activity in pancreatic cancers.
S7748 EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
MedComm (2020), 2025, 6(6):e70150
Cell Rep, 2024, 43(11):114930
Oncogene, 2024, 10.1038/s41388-024-03049-6
Verified customer review of EPZ015666 (GSK3235025)
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
S8111 GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
J Immunother Cancer, 2025, 13(4)e011299
J Clin Invest, 2024, e175023
Cancer Lett, 2024, 604:217263
Verified customer review of GSK591
S8624 Onametostat (JNJ-64619178) Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
Sci Rep, 2024, 14(1):4303
SLAS Discov, 2024, 29(4):100161
S7884 AMI-1 AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
Cell Death Dis, 2023, 14(4):233
Oncogenesis, 2022, 11(1):45
Oncogene, 2021, 40(7):1375-1389
Verified customer review of AMI-1
S7832 SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
Cell Death Dis, 2022, 13(11):943
J Med Chem, 2020, 31
Transpl Int, 2020, 33(2):229-243
S8147 MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
Theranostics, 2024, 14(10):4090-4106
Front Cell Dev Biol, 2021, 9:741736
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S7820 EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Theranostics, 2024, 14(10):4090-4106
Nat Commun, 2023, 14(1):1430
Inflamm Res, 2022, 71(3):309-320
S8340 SGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.
Clin Exp Med, 2025, 25(1):102
Redox Biol, 2024, 78:103414
Cell Rep, 2022, 39(12):110994
S8209 HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
Front Immunol, 2019, 10:174
Nat Commun, 2018, 9(1):1572
Cancer Res, 2018, 78(20):5731-5740
S5445 AMI-1 (free acid) AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.