KT-333 是同类首创、强效且选择性的异双功能STAT3降解剂,可募集VHL E3连接酶进行泛素-蛋白酶体介导的降解。它在ALK⁺间变性大细胞淋巴瘤 (ALCL) 的临床前模型中诱导出强大的抗肿瘤活性。
MoreUpadacitinib是选择性JAK1抑制剂,对JAK1和JAK2的IC50值分别为0.045 μM和0.109 μM,而对JAK3和TYK2的IC50值分别为2.1 μM和4.7 μM
MorePemrametostat (GSK3326595, EPZ015938)是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5 (PRMT5)抑制剂,在体内外有效地抑制肿瘤生长。
MoreRalometostat (TNG908) is a potent, selective, and brain-penetrant PRMT5 inhibitor with an IC50 of 4 μM, exerting its effect through an MTA synergistic mechanism. It also demonstrates antitumor activity in xenograft models.
MoreMRTX1719 is a potent and selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5·MTA), which serves as a potential selective therapeutic target for tumor intervention.
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