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Chemical Structure : CSN5i-3
CAS No.: 2375740-98-8
Catalog No.: PC-61193Not For Human Use, Lab Use Only.
CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $328 | In stock | |
| 2 mg | $528 | In stock | |
| 5 mg | $958 | In stock | |
| 10 mg | Get quote | ||
| 25 mg | Get quote |
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CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN).
CSN5i-3 displays >1,000-fold selectivity over JAMM domain proteases (Rpn11 and AMSHLP) and other metalloproteinases.
CSN5i-3 inhibits CSN-catalysed Cul1 deneddylation with IC50 of 5.8 nM, traps the cullin-RING E3 ubiquitin ligases (CRLs) in the neddylated state, and results in the inactivation of a subset of CRLs and the stabilization of their substrates.
CSN5i-3 exhibits a differentiating effect on the viability of cancer cells, inhibits growth of a human xenograft in vivo.
| M.Wt | 505.57 | |
| Formula | C28H29F2N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(difluoromethyl)-N-(6-((5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl)-[1,1'-biphenyl]-3-yl)-1-isopropyl-1H-pyrazole-5-carboxamide |
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1. Schlierf A, et al. Nat Commun. 2016 Oct 24;7:13166.
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