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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | 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 5.8u2009nM. |
Storage Temp | Protected from light,Store at -20°C,Argon charged |
Shipped In | Ice 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) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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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 |
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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 |
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Solubility | DMSO : ≥ 100 mg/mL (197.80 mM) |
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