PRMT5 选择性抑制剂

目录号 产品名 产品描述 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)是一种有效的、选择性PRMT5抑制剂。

Selective PRMT5, IC50: 4 nM
S7748 EPZ015666 (GSK3235025)

EPZ015666(GSK3235025) 是一种有效的,选择性且口服生物有效的 PRMT5 抑制剂,Ki 为 5 nM,选择性比其它 PMTs 高 20,000多倍。

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是一种有效的、选择性PRMT5抑制剂,用作治疗急性髓性白血病。

Selective PRMT5, IC50: 16.74 μM