CSN5i-3( CSN5 inhibitor 3 )

Catalog No. M17001 CAS No. ——

COA

Datasheet

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Product Name

CSN5i-3
Note

Research use only, not for human use.
Brief Description

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).
Description

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); displays >1,000-fold selectivity over JAMM domain proteases (Rpn11 and AMSHLP) and other metalloproteinases; 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; exhibits a differentiating effect on the viability of cancer cells, inhibits growth of a human xenograft in vivo.
In Vitro

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In Vivo

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Synonyms

CSN5 inhibitor 3
Pathway

Proteasome/Ubiquitin
Target

Proteasome
Recptor

Proteasome
Research Area

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Indication

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CAS Number

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Formula Weight

505.57
Molecular Formula

C28H29F2N5O2
Purity

>98% (HPLC)
Solubility

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SMILES

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Chemical Name

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

1. Schlierf A, et al. Nat Commun. 2016 Oct 24;7:13166.

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