CSN5i-3
目录号: PL08517 纯度: ≥99%
CSN5i-3 是一种有效的,选择性和口服的 CSN5/Jab1 抑制剂,抑制 CSN 催化的 Cul1 deneddylation IC50 值为 5.8 nM。
CAS No. :2375740-98-8
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中文名称
CSN5i-3
英文名称
CSN5i-3
英文别名
CSN5i-3;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;BDBM50514114;Chembl4528101
Cas No.
2375740-98-8
分子式
C28H29F2N5O2
分子量
505.56
包装储存
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
CSN5i-3 是一种有效的,选择性和口服的 CSN5/Jab1 抑制剂,抑制 CSN 催化的 Cul1 deneddylation IC50 值为 5.8 nM。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
IC50: 5.8 nM (CSN5)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (197.80 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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