CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1 , and inhibits CSN-catalysed Cul1 deneddylation with an IC 50 value of 5.8 nM In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 5.8 nM (CSN5)
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CSN5i-3
CAS number:2375740-98-8 molecular formula:C28H29F2N5O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2375740-98-8 | molecular formula | C28H29F2N5O2 |
| molecular weight | 505.56 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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