THAL-SNS-032 是一种选择性的 Cyclin-dependent kinase 9 (CDK9) 的降解剂PROTAC,包含一个与CDK结合的SNS-032配体、一个thalidomide衍生物和 E3 ubiquitin ligase Cereblon (CRBN)相结合
MoreSimurosertib (TAK-931) 是一种具有口服活性,选择性, ATP 竞争性的细胞分裂周期 7 (CDC7) 激酶抑制剂,IC50 为 <0.3 nM。Simurosertib 具有抗癌活性。
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.
MoreOnametostat (JNJ-64619178)是PRMT5抑制剂,具有较高的选择性和效力(PRMT5-MEP-50, IC50=0.14 nM)、良好的药代动力学特性以及安全性
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