CSN5i-3

Tocris Bioscience | Catalog # 7089

Potent and selective CSN5 (COP9 signalosome) inhibitor
Tocris Bioscience

Key Product Details

Description

Potent and selective CSN5 (COP9 signalosome) inhibitor
View all Ubiquitin Ligase (E3) Inhibitors »

Product Description

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.

Scientific Data Images for CSN5i-3

Novartis vs Bio-Techne batch comparison for CSN5i-3

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.

Product Specifications for CSN5i-3

Molecular Weight

505.57

Formula

C28H29F2N5O2

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

CAS Number

2375740-98-8

PubChem ID

129892190

InChI Key

ANNKHJQLDMGQFM-UIOOFZCWSA-N

SMILES

CC(N1N=C(C(F)F)C=C1C(NC2=CC(C3=CC=CC=C3)=C([C@H]4[C@H](CCCC5=CN=CN45)O)C=C2)=O)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.56 100

Preparing Stock Solutions for CSN5i-3

The following data is based on the product molecular weight 505.57.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.98 mL 9.89 mL 19.78 mL
5 mM 0.40 mL 1.98 mL 3.96 mL
10 mM 0.20 mL 0.99 mL 1.98 mL
50 mM 0.04 mL 0.20 mL 0.40 mL

Calculators

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Background References

References are publications that support the biological activity of the product.

Product Documents for CSN5i-3

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for CSN5i-3

For research use only

Related Research Areas

E3 Ubiquitin Ligases

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