| Identification | Back Directory | [Name]
1H-Pyrazole-5-carboxamide, 3-(difluoromethyl)-1-(1-methylethyl)-N-[6-[(5S,6S)-6,7,8,9-tetrahydro-6-hydroxy-5H-imidazo[1,5-a]azepin-5-yl][1,1'-biphenyl]-3-yl]- | [CAS]
2375740-98-8 | [Synonyms]
1H-Pyrazole-5-carboxamide, 3-(difluoromethyl)-1-(1-methylethyl)-N-[6-[(5S,6S)-6,7,8,9-tetrahydro-6-hydroxy-5H-imidazo[1,5-a]azepin-5-yl][1,1'-biphenyl]-3-yl]- | [Molecular Formula]
C28H29F2N5O2 | [MDL Number]
MFCD31657416 | [MOL File]
2375740-98-8.mol | [Molecular Weight]
505.56 |
| Chemical Properties | Back Directory | [Boiling point ]
666.5±55.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO:50.56(Max Conc. mg/mL);100.0(Max Conc. mM) | [form ]
Solid | [pka]
12.66±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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[1]. | [storage]
Store at -20°C, protect from light, stored under nitrogen | [References]
[1] Schlierf A, et al. Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166. DOI:10.1038/ncomms13166 |
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