CSN5i-3 B( —— )

Catalog No. M32870 CAS No. 2375740-98-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CSN5i-3 B
Note

Research use only, not for human use.
Brief Description

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5.
Description

CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8?nM.
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.
In Vivo

CSN5i-3 shows a good pharmacokinetic profile. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction.
Synonyms

——
Pathway

Apoptosis
Target

Apoptosis
Recptor

Apoptosis
Research Area

——
Indication

——

CAS Number

2375740-98-8
Formula Weight

505.56
Molecular Formula

C28H29F2N5O2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : ≥ 100 mg/mL (197.80 mM)
SMILES

CC(C)n1nc(cc1C(=O)Nc1ccc([C@H]2[C@@H](O)CCCc3cncn23)c(c1)-c1ccccc1)C(F)F
Chemical Name

——

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

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