产品
编 号:F618401
分子式:C28H29F2N5O2
分子量:505.56
产品类型
结构图
CAS No: 2375740-98-8
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产品详情
生物活性:
CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8?nM.
体内研究:
CSN5i-3 shows a good pharmacokinetic profile. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction.
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.