[CAS NO. 2375740-98-8] CSN5i-3
PRODUCTS SPECIFICATIONS [2375740-98-8]
DESCRIPTION [2375740-98-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 505.56 |
| Molecular Formula | C28H29F2N5O2 |
| SMILES | O=C(C1=CC(C(F)F)=NN1C(C)C)NC2=CC(C3=CC=CC=C3)=C([C@@H]4N5C(CCC[C@@H]4O)=CN=C5)C=C2 |
3 Publications Citing Use of MCE
Summary
CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1 , and inhibits CSN-catalysed Cul1 deneddylation with an IC 50 value of 5.8 nM [1] .
IC50 & Target
IC50: 5.8 nM (CSN5) [1]
In Vitro
CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CSN5i-3 shows a good pharmacokinetic profile. CSN5i-3 inhibits growth of human xenograft. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 197.80 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9780 mL | 9.8900 mL | 19.7800 mL |
| 5 mM | 0.3956 mL | 1.9780 mL | 3.9560 mL |
| 10 mM | 0.1978 mL | 0.9890 mL | 1.9780 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution