Chemical Name: 3-(Difluoromethyl)-N-(6-((5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl)-[1,10-biphenyl]-3-yl)-1-isopropyl-1H-pyrazole-5-carboxamide
Biological ActivityCSN5i-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.
Novartis vs Bio-Techne batch comparison for CSN5i-3 Effects of CSN5i-3 on a cancer cell line. (A) Concentration dependent effects (t = 3 days) of CSN5i-3. The IC50 values are 26 nM and 16 nM for Novartis batch and Bio-Techne batch, respectively. (B) Cullins Cul4A level after treatment (t = 2 hours) with 100 nM of CSN5i-3 from either Novartis or Bio-Techne.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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