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Ralometostat (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.
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MRTX1719 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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Copanlisib是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3.
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Inavolisib (GDC-0077, RG6114, RO-7113755) 是一种有效的 PI3K alpha (PI3Kα) 选择性抑制剂，IC50 为 0.038 nM。GDC-0077 对 PI3K α 的选择性比其他 I 类 PI3K 异构体（β、δ 和 γ）高 300 倍以上，对 PIK 家族成员的选择性高 2000 倍以上。GDC-0077 可与 PI3K 的 ATP 结合位点结合并抑制 PIP2 磷酸化为 PIP3
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Zimlovisertib (PF-06650833)是一种有效的IRAK4选择性抑制剂，IC50为0.2 nM
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