生物活性
CSN5i-3 是一种有效的,选择性和口服的 CSN5/Jab1 抑制剂,抑制 CSN 催化的 Cul1 deneddylation IC50 值为 5.8 nM。
靶点
IC50: 5.8 nM (CSN5)
体外研究
CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module.
体内研究
CSN5i-3 shows a good pharmacokinetic profile. CSN5i-3 inhibits growth of human xenograft. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction.
青岛恺润生物医药科技有限公司
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