PRMT5 Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
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.
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|
GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
|Selective||PRMT5, IC50: 4 nM|
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|
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|
HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
|Selective||PRMT5, IC50: 16.74 μM|
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