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Tocris Bioscience™ CSN5i-3
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Catalog No. 70892
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70-892 2 mg
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Catalog No. 70-892 Supplier Tocris Bioscience™ Supplier No. 7089/2
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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
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