PRMT

Inhibitory Selectivity

Isoform-specific Inhibitors

PRMT Products

All (17) PRMT Inhibitors (16)

Catalog No.	Information	Product Use Citations	Product Validations
S7748	EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with K_i of 5 nM, >20,000-fold selectivity over other PMTs.	Sci Adv, 2021, 7(13)eabc1834 Front Immunol, 2021, 12:695947 Proc Natl Acad Sci U S A, 2020, 117(45):28068-28079	(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
S8147	MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.	EMBO Rep, 2020, 21(2):e48597
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.
S7820	EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.	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 K_d 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
S0855^New	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.
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.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389 Proteome Sci, 2020, 19;18:6
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.
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.
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 Oncogene, 2019, 38(46):7181-7195 Cancer Med, 2019, 8(5):2414-2428
S8111	GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.	Elife, 2020, 9e57617 J Immunother Cancer, 2019, 7(1):277 Cancer Res, 2018, 78(20):5731-5740	Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
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
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.
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 Ki^app vaules ranging from 1.5 to 81 nM.
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 Cell Rep, 2018, 24(12):3207-3223	Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
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
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.

Catalog No.	Information	Product Use Citations	Product Validations
S7748	EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with K_i of 5 nM, >20,000-fold selectivity over other PMTs.	Sci Adv, 2021, 7(13)eabc1834 Front Immunol, 2021, 12:695947 Proc Natl Acad Sci U S A, 2020, 117(45):28068-28079	(B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.
S8147	MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.	EMBO Rep, 2020, 21(2):e48597
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.
S7820	EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.	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 K_d 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
S0855^New	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.
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.	Oncogene, 2021, 10.1038/s41388-020-01617-0 Oncogene, 2021, 40(7):1375-1389 Proteome Sci, 2020, 19;18:6
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.
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.
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 Oncogene, 2019, 38(46):7181-7195 Cancer Med, 2019, 8(5):2414-2428
S8111	GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.	Elife, 2020, 9e57617 J Immunother Cancer, 2019, 7(1):277 Cancer Res, 2018, 78(20):5731-5740	Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.
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
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.
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 Ki^app vaules ranging from 1.5 to 81 nM.
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 Cell Rep, 2018, 24(12):3207-3223	Effects of microinjection of AMI-1 into the RVLM on cardiovascular activity in the Ang II-induced hypertensive rats. The representative original tracings (A)
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

Catalog No.	Information	Product Use Citations	Product Validations
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.

Catalog No.

Information

Product Use Citations

Product Validations

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.

Choose Your Country or Region

By Signaling Pathways

By product type

PRMT

Inhibitory Selectivity

Isoform-specific Inhibitors

PRMT Products