CSN5i-3 | CSN5 inhibitor | Probechem Biochemicals

Chemical Structure : CSN5i-3

CAS No.: 2375740-98-8

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CSN5i-3 (CSN5 inhibitor 3)

货号: PC-61193Not For Human Use, Lab Use Only.

CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN).

规格	价格	库存
1 mg	￥3280	In stock
2 mg	￥5280	In stock
5 mg	￥9580	In stock
10 mg		Get quote
25 mg		Get quote

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生物&药学活性

CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN).
CSN5i-3 displays >1,000-fold selectivity over JAMM domain proteases (Rpn11 and AMSHLP) and other metalloproteinases.
CSN5i-3 inhibits CSN-catalysed Cul1 deneddylation with IC50 of 5.8 nM, traps the cullin-RING E3 ubiquitin ligases (CRLs) in the neddylated state, and results in the inactivation of a subset of CRLs and the stabilization of their substrates.
CSN5i-3 exhibits a differentiating effect on the viability of cancer cells, inhibits growth of a human xenograft in vivo.

物理化学性质&存储条件

分子量	505.57
分子式	C28H29F2N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Schlierf A, et al. Nat Commun. 2016 Oct 24;7:13166.

CSN5i-3 (CSN5 inhibitor 3)

生物&药学活性

物理化学性质&存储条件

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CSN5i-3 (CSN5 inhibitor 3)

生物&药学活性

物理化学性质&存储条件

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