Tocris Bioscience™ CSN5i-3

Description

Potent and selective CSN5 (COP9 signalosome) inhibitor

CSN5i-3 is a potent and selective CSN5 (COP9 signalosome) inhibitor. It inhibits deneddylation of NEDD8-modifed CRLs (IC50 = 5.8 nM), keeping them in the neddylated state, and leading to inactivation of a subset of CRLs by inducing degradation of their substrate receptor module (SRM). In A2780 ovarian cancer cells, CSN5i-3 down-regulates the expression of COPS5 and arrest cells at S-phase. In HUVECs in vitro and in zebrafish embryos in vivo, CSN5i-3 induces endothelial barrier disruption and increases macromolecule leakage by increasing the expression and activity of RhoGTPases. CSN5i-3 also inhibits the growth of lymphoma cell xenografts in mice. Orally bioavailable.

The negative control CSN5i-3-NEG (Cat. No. 7532) is also available.

Specifications

• Chemical Name or Material: 3-(Difluoromethyl)-N-(6-((5 S,6 S)-6-hydroxy-6,7,8,9-tetrahydro-5 H-imidazo[1,5-a]azepin-5-yl)-[1,10-biphenyl]-3-yl)-1-isopropyl-1 H-pyrazole-5-carboxamide
• CAS: 2375740-98-8
• Quantity: 2 mg
• Target: Ubiquitin Ligase (E3) Inhibitors
• Molecular Formula: C₂₈H₂₉F₂N₅O₂
• Purity: 0.98