You are here:Home-Chemical Inhibitors & Agonists-Proteasome/Ubiquitin-Proteasome-CSN5i-3
CSN5i-3

Chemical Structure : CSN5i-3

CAS No.: 2375740-98-8

CSN5i-3 (CSN5 inhibitor 3)

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
50 mg Get quote
100 mg Get quote
500 mg Get quote
1 g Get quote

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 505.57
    Formula C28H29F2N5O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    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

    References

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

    Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

    Contact Us sales@probechem.com

    Bulk Inquiry

    * Indicates a Required FieldYour information is safe with us.

    • *Product name:
    • *Applicant name:
    • *Email address:
    • *Organization name:
    • *Requested quantity:
    • *Country:
    • *Additional Information:

    Get Quote

    * Indicates a Required FieldYour information is safe with us.

    • *Product name:
    • *Applicant name:
    • *Email address:
    • *Organization name:
    • *Requested quantity:
    • *Country:
    • Additional Information: