CSN5i-3

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CSN5i-3

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

规格:	98%
分子量:	505.56

包装与价格：

包装	价格(元)
1mg	询价
5mg	询价
10mg	询价

CSN5i-3是一种有效的，选择性和口服的CSN5抑制剂;抑制CSN催化的Cul1deneddylationIC50值为5.8nM。
货号:ajcx13402
CAS:2375740-98-8
分子式:C28H29F2N5O2
分子量：505.56
溶解度:DMSO: ≥ 100 mg/mL (197.80 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

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[1].

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[1].

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

Protocol:

Cell experiment:

Cell viability is measured using the CellTiter-Glo Assay. Cells (THP-1, HCT116, NCI-H2030 and TE-1) are treated with CSN5i-3 (1 nM, 10 nM, 100 nM, 1 μM, 10 μM) for 72 hours[1].

Animal experiment:

Mice[1]SU-DHL-1 xenografts were grown in SCID-bg mice and dosed by oral administration with either vehicle control or CSN5i-3 at the indicated doses (50 mg/kg BID, 100mg/kg QD) and schedules (3, 7, 10, 14 day). Tumour response is reported as percentage change in tumour volume at the last day of treatment relative to start of treatment.

参考文献:

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