PRMT

Inhibitory Selectivity

PRMT Products

All (16) PRMT Inhibitors (15)

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.	Proc Natl Acad Sci U S A, 2020, 117(45):28068-28079 Signal Transduct Target Ther, 2020, 5(1):197 Theranostics, 2019, 9(9):2606-2617	(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 J Immunother Cancer, 2019, 7(1):277
S8883^New	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.
S8858^New	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.
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 Proteome Sci, 2020, 19;18:6
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	GSK3326595 (EPZ015938) 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.	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 Med, 2018, 7(3):869-882	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
S8624	JNJ-64619178 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.
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 Cell Rep, 2018, 24(12):3207-3223 Nitric Oxide, 2017, 67:58-67	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
S0184^New	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.	Proc Natl Acad Sci U S A, 2020, 117(45):28068-28079 Signal Transduct Target Ther, 2020, 5(1):197 Theranostics, 2019, 9(9):2606-2617	(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 J Immunother Cancer, 2019, 7(1):277
S8883^New	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.
S8858^New	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.
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 Proteome Sci, 2020, 19;18:6
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	GSK3326595 (EPZ015938) 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.	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 Med, 2018, 7(3):869-882	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
S8624	JNJ-64619178 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.
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 Cell Rep, 2018, 24(12):3207-3223 Nitric Oxide, 2017, 67:58-67	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

Catalog No.	Information	Product Use Citations	Product Validations
S0184^New	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^New

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.

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PRMT

Inhibitory Selectivity

PRMT Products

EPZ015666 (GSK3235025)

MS049

SGC2085

EPZ020411 2HCl

SGC707

LLY-283

GSK3368715 (EPZ019997) 3HCl

MS023

AMI-1 (free acid)

GSK3326595 (EPZ015938)

GSK591

HLCL-61 HCL

JNJ-64619178

AMI-1

C7280948

XY1