PRMT

Inhibitory Selectivity

PRMT Products

Catalog No. Information Product Use Citations Product Validations
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.

S8147

MS049

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.

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.

S8479

LLY-283

LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.

S7820

EPZ020411 2HCl

EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.

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.

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.

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.

S8111

GSK591

GSK591 (EPZ015866,GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.

S8209

HLCL-61 HCL

HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.

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.

Catalog No. Information Product Use Citations Product Validations
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.

S8147

MS049

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.

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.

S8479

LLY-283

LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.

S7820

EPZ020411 2HCl

EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.

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.

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.

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.

S8111

GSK591

GSK591 (EPZ015866,GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.

S8209

HLCL-61 HCL

HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.

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.

Tags: PRMT inhibitor | PRMT activator | PRMT inhibition