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CSN5i-3

Catalog No. T10895   CAS 2375740-98-8

CSN5i-3 is a novel potent oral and selective CSN5/Jab1 inhibitor that inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM.CSN5i-3 exhibits anticancer activity, inhibits cell proliferation and induces apoptosis in human breast cancer cells.

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CSN5i-3 Chemical Structure
CSN5i-3, CAS 2375740-98-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 378.00
5 mg In stock $ 813.00
10 mg In stock $ 1,230.00
25 mg In stock $ 1,830.00
50 mg In stock $ 2,470.00
100 mg In stock $ 3,330.00
1 mL * 10 mM (in DMSO) In stock $ 886.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CSN5i-3 is a novel potent oral and selective CSN5/Jab1 inhibitor that inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM.CSN5i-3 exhibits anticancer activity, inhibits cell proliferation and induces apoptosis in human breast cancer cells.
Targets&IC50 CSN5:5.8 nM
In vitro CSN5i-3, by trapping CRLs in the neddylation state, effectively causes the inactivation of a specific subset of CRLs through the induction of degradation in their substrate recognition module.[1]
In vivo CSN5i-3 exhibits a favorable pharmacokinetic profile, and its application results in the formation of cleaved PARP and cleaved caspase 3, indicating the initiation of apoptosis.[1]
Molecular Weight 505.56
Formula C28H29F2N5O2
CAS No. 2375740-98-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 75.83 mg/mL (150 mM)

TargetMolReferences and Literature

1. Schlierf A, et al. Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library

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Keywords

CSN5i-3 2375740-98-8 Apoptosis Others CSN5i3 CSN-5i-3 CSN5i 3 inhibitor inhibit

 

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