生物活性
CSN5i-3 是一種有效的,選擇性和口服的 CSN5/Jab1 抑制劑,抑制 CSN 催化的 Cul1 deneddylation IC50 值為 5.8 nM。
靶點(diǎn)
IC50: 5.8 nM (CSN5)
體外研究
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.
體內(nèi)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.
青島愷潤生物醫(yī)藥科技有限公司
聯(lián)系商家時(shí)請?zhí)峒癱hemicalbook,有助于交易順利完成!
微信洽談