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BC-1215

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Chemical Structure| 1507370-20-8 同义名 : -
CAS号 : 1507370-20-8
货号 : A1173075
分子式 : C26H26N4
纯度 : 99%+
分子量 : 394.512
MDL号 : MFCD28118991
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
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.
实验方案
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