PRMT5 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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.

Selective
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.

Selective PRMT5, IC50: 0.14 nM
S8111 GSK591

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

Selective PRMT5, IC50: 4 nM
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.

Selective PRMT5, Ki: 5 nM
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.

Selective PRMT5, IC50: 25 nM; PRMT5, IC50: 22 nM
S8209 HLCL-61 HCL

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

Selective PRMT5, IC50: 16.74 μM