CSN5i-3 - 99%, high purity , CAS No.2375740-98-8

  • ≥99%
Item Number
C648681
Grouped product items
SKUSizeAvailabilityPrice Qty
C648681-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$550.90
C648681-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$980.90
C648681-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,500.90

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsCSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1 , and inhibits CSN-catalysed Cul1 deneddylation with an IC 50 value of 5.8u2009nM.
Storage TempProtected from light,Store at -20°C,Argon charged
Shipped InIce chest + Ice pads
Product Description

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

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. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:IC50: 5.8 nM (CSN5)

Associated Targets(Human)

COPS5 Tchem COP9 signalosome complex subunit 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 5-(difluoromethyl)-N-[4-[(5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl]-3-phenylphenyl]-2-propan-2-ylpyrazole-3-carboxamide
INCHI InChI=1S/C28H29F2N5O2/c1-17(2)35-24(14-23(33-35)27(29)30)28(37)32-19-11-12-21(22(13-19)18-7-4-3-5-8-18)26-25(36)10-6-9-20-15-31-16-34(20)26/h3-5,7-8,11-17,25-27,36H,6,9-10H2,1-2H3,(H,32,37)/t25-,26-/m0/s1
InChi Key ANNKHJQLDMGQFM-UIOOFZCWSA-N
Canonical SMILES CC(C)N1C(=CC(=N1)C(F)F)C(=O)NC2=CC(=C(C=C2)C3C(CCCC4=CN=CN34)O)C5=CC=CC=C5
Isomeric SMILES CC(C)N1C(=CC(=N1)C(F)F)C(=O)NC2=CC(=C(C=C2)[C@H]3[C@H](CCCC4=CN=CN34)O)C5=CC=CC=C5
PubChem CID 129892190
MeSH Entry Terms 3-(difluoromethyl)-N-(6-((5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo(1,5-a)azepin-5-yl)-(1,1'-biphenyl)-3-yl)-1-isopropyl-1H-pyrazole-5-carboxamide;CSN5 inhibitor 3;CSN5i-3
Molecular Weight 505.56

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : ≥ 100 mg/mL (197.80 mM)

Related Documents

Solution Calculators