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PRMT

Isoform-selective Products

PRMT5 PRMT4 PRMT6 PRMT1 PRMT8 PRMT3

PRMT Products

All (27)
PRMT Inhibitors (25)
New PRMT Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Oncogene, 2024, 10.1038/s41388-024-03049-6 Elife, 2024, 12RP89754 SLAS Discov, 2024, 29(4):100161
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.	NPJ Precis Oncol, 2024, 8(1):52 Elife, 2024, 12RP90683 J Med Chem, 2024, 67(8):6064-6080.
S8111	GSK591	GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.	J Clin Invest, 2024, e175023 Cancer Lett, 2024, 604:217263 Heliyon, 2024, 10(19):e37958
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.	J Immunother Cancer, 2024, 12(9)e009603 Mol Oncol, 2024, 10.1002/1878-0261.13725 Sci Rep, 2024, 14(1):4303
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
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.	Cell Death Dis, 2022, 13(11):943 J Med Chem, 2020, 31 Transpl Int, 2020, 33(2):229-243
S6737	C7280948	C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.	Cell Death Dis, 2023, 14(4):233 Cell Death Dis, 2023, 14(8):512 Cell Death Dis, 2023, 14(8):512
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.	Sci Rep, 2024, 14(1):4303 SLAS Discov, 2024, 29(4):100161 Nat Commun, 2023, 14(1):1078
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 Ki^app 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
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.	Nat Commun, 2023, 14(1):1078 J Pharm Anal, 2023, 13(6):590-602 Ecotoxicol Environ Saf, 2022, 243:113992
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
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
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 Research Square, 2021, 10.21203/rs.3.rs-620216/v1 EMBO Rep, 2020, 21(2):e48597
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.	Mol Ther, 2023, 10.1016/j.ymthe.2023.09.011 Cell Death Dis, 2023, 14(4):233
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.	Cell Rep, 2022, 39(12):110994
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.
S8479	LLY-284	LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283.
E1600^New	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.
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.
E1024	MRTX1719	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.
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.
E4701^New	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.
E1349^New	TNG908	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.
E1658^New	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.
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
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 K_i of 5 nM, >20,000-fold selectivity over other PMTs.	Oncogene, 2024, 10.1038/s41388-024-03049-6 Elife, 2024, 12RP89754 SLAS Discov, 2024, 29(4):100161
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.	NPJ Precis Oncol, 2024, 8(1):52 Elife, 2024, 12RP90683 J Med Chem, 2024, 67(8):6064-6080.
S8111	GSK591	GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.	J Clin Invest, 2024, e175023 Cancer Lett, 2024, 604:217263 Heliyon, 2024, 10(19):e37958
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.	J Immunother Cancer, 2024, 12(9)e009603 Mol Oncol, 2024, 10.1002/1878-0261.13725 Sci Rep, 2024, 14(1):4303
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
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.	Cell Death Dis, 2022, 13(11):943 J Med Chem, 2020, 31 Transpl Int, 2020, 33(2):229-243
S6737	C7280948	C7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 12.8 μM in vitro.	Cell Death Dis, 2023, 14(4):233 Cell Death Dis, 2023, 14(8):512 Cell Death Dis, 2023, 14(8):512
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.	Sci Rep, 2024, 14(1):4303 SLAS Discov, 2024, 29(4):100161 Nat Commun, 2023, 14(1):1078
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 Ki^app 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
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.	Nat Commun, 2023, 14(1):1078 J Pharm Anal, 2023, 13(6):590-602 Ecotoxicol Environ Saf, 2022, 243:113992
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
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
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 Research Square, 2021, 10.21203/rs.3.rs-620216/v1 EMBO Rep, 2020, 21(2):e48597
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.	Mol Ther, 2023, 10.1016/j.ymthe.2023.09.011 Cell Death Dis, 2023, 14(4):233
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.	Cell Rep, 2022, 39(12):110994
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.
E1600^New	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.
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.
E1024	MRTX1719	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.
E4701^New	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.
E1349^New	TNG908	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.
E1658^New	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.
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
E1429	T1-44	T1-44 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits anti-tumor activity in pancreatic cancers.
E1600^New	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.
E4701^New	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.
E1349^New	TNG908	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.
E1658^New	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.

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Tags: PRMT inhibitor | PRMT activator | PRMT inhibition