规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50μL*10mM(DMSO) | ¥99随货¥69 | 咨询 | |
100μL*10mM(DMSO) | ¥109随货¥79 | 咨询 | |
250μL*10mM(DMSO) | ¥129随货¥99 | 咨询 | |
500μL*10mM(DMSO) | ¥239随货¥169 | 咨询 | |
10mM*1mL(DMSO) | ¥328 | 咨询 | |
1mg | ¥176 | 咨询 | |
5mg | ¥378 | 咨询 | |
10mg | ¥605 | 咨询 | |
25mg | ¥998 | 咨询 | |
50mg | ¥1398 | 咨询 | |
100mg | ¥1957 | 咨询 |
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描述 | Fbxo3 is a ubiquitin E3 ligase F box component, which potently stimulates cytokine secretion from human inflammatory cells by mediating the degradation of the TRAF inhibitory protein, Fbxl2. BC-1215 is a highly unique, selective Fbxo3 inhibitor with an estimated IC50 value of 10-7M, measured by prevention of SCFFbxo3 catalyzed Fbxl2 ubiquitination in vitro. BC-1215 exhibited maximal inhibitory binding at 10-7M, measured by quantification of bound Fbxl2 protein. As the inhibition of Fbxo3, the known Fbxl2 substrates including cyclin D2, cyclin D3, and cytidylyl-transferase were decreased in MLE cells treated with BC-1215 at 10μM and 50μM for 16h. The suppression of upregulated levels of TRAF2 and TRAF3, along with activating the downstream p38 and phospho-IKK in the NF-kB pathway, by TNF treatment could also be observed in MLE cells treated with 10μg/ml BC-1215 for 6h. BC-1215 reversibly inhibited Fbxo3 resulting in destabilized TRAF proteins. Intraperitoneal injection with BC-1215 at doses of 0.8, 4, 20, 100 and 500μg/kg, 10 minutes prior to LPS challenge, dose-dependently inhibited the release of IL-1b, IL-6, and TNF-α in blood of mice. In vivo administration of BC-1215 effectively lessened the severity of viral pneumonia, septic shock, colitis, and cytokine-driven inflammation systemically in murine models. |
计算器 | ||||
存储液制备 | ![]() | 1mg | 5mg | 10mg |
1 mM 5 mM 10 mM | 2.53mL 0.51mL 0.25mL | 12.67mL 2.53mL 1.27mL | 25.35mL 5.07mL 2.53mL |
CAS号 | 1507370-20-8 |
分子式 | C26H26N4 |
分子量 | 394.512 |
别名 | |
运输 | 蓝冰 |
存储条件 | In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,2-8°C |
溶解方案 | DMSO: 1 mg/mL(2.53 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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