CSN5i-3
Tocris Bioscience, part of Bio-Techne | Catalog # 7089
Potent and selective CSN5 (COP9 signalosome) inhibitor
Key Product Details
Description
Potent and selective CSN5 (COP9 signalosome) inhibitor
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
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Zhange COPS5 inhibition arrests the proliferation and growth of serous ovarian cancer cells via the elevation of p27 level. Biochem.Biophys.Res.Commun. 2017 PMID: 28919423
- Majolée CSN5 inhibition triggers inflammatory signaling and Rho/ROCK-dependent loss of endothelial integrity. Sci.Rep. 2019 PMID: 31148579
- Schlierf Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat.Commun. 2016 PMID: 27774986
Product Specific Notices for CSN5i-3
For research use only
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