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  • PRMT Inhibitors (18)
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Catalog No. Product Name Information Product Use Citations Product Validations
E1007New 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.
E1088New 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.
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. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.
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.
S6737 C7280948 C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
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.
Sci Adv, 2021, 7(13)eabc1834
Front Immunol, 2021, 12:695947
Ann Transl Med, 2021, 9(9):755
S7820New EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Inflamm Res, 2022, 71(3):309-320
Theranostics, 2020, 10(1):133-150
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.
J Med Chem, 2020, 31
Transpl Int, 2020, 33(2):229-243
J Immunother Cancer, 2019, 7(1):277
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.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S8111 GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Cancer Sci, 2021, 10.1111/cas.14988
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.
Sci Adv, 2022, 8(4):eabi7711
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
S8147 MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
EMBO Rep, 2020, 21(2):e48597
S8209 HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
Nat Commun, 2018, 9(1):1572
Cancer Res, 2018, 78(20):5731-5740
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.
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.
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
S8664 Pemrametostat (GSK3326595) 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.
Sci Adv, 2021, 7(13)eabc1834
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
Cell Chem Biol, 2021, S2451-9456(21)00400-1
S8858 GSK3368715 (EPZ019997) 3HCl GSK3368715 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.
Mol Cell Biol, 2022, e0052321
S8883 LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
J Clin Lab Anal, 2022, e24176
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.
E1007New 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.
E1088New 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.
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. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.
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.
S6737 C7280948 C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
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.
Sci Adv, 2021, 7(13)eabc1834
Front Immunol, 2021, 12:695947
Ann Transl Med, 2021, 9(9):755
S7820New EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Inflamm Res, 2022, 71(3):309-320
Theranostics, 2020, 10(1):133-150
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.
J Med Chem, 2020, 31
Transpl Int, 2020, 33(2):229-243
J Immunother Cancer, 2019, 7(1):277
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.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S8111 GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Cancer Sci, 2021, 10.1111/cas.14988
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.
Sci Adv, 2022, 8(4):eabi7711
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
S8147 MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
EMBO Rep, 2020, 21(2):e48597
S8209 HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
Nat Commun, 2018, 9(1):1572
Cancer Res, 2018, 78(20):5731-5740
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.
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.
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
S8664 Pemrametostat (GSK3326595) 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.
Sci Adv, 2021, 7(13)eabc1834
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
Cell Chem Biol, 2021, S2451-9456(21)00400-1
S8858 GSK3368715 (EPZ019997) 3HCl GSK3368715 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.
Mol Cell Biol, 2022, e0052321
S8883 LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
J Clin Lab Anal, 2022, e24176
E1007New 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.
E1088New 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.
S7820New EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Inflamm Res, 2022, 71(3):309-320
Theranostics, 2020, 10(1):133-150
Tags: PRMT inhibitor | PRMT activator | PRMT inhibition