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FLI-06

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Chemical Structure| 313967-18-9 同义名 : -
CAS号 : 313967-18-9
货号 : A123790
分子式 : C25H30N2O5
纯度 : 99%+
分子量 : 438.516
MDL号 : MFCD00330996
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: 40 mg/mL(91.22 mM)，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 Notch signaling plays an important role in regulating gene transcription involved in cell fate, cell differentiation, and tissue homeostasis. FLI-06 is an inhibitor of Notch signaling with an EC50 value of 2.3 ± 0.8 μM. Incubation of 10 μM FLI-06 for 16 hours resulted in aberrant glycosylation in HEK293 cells stably expressing Klotho. Treatment of C2C12 cells with 10 μM FLI-06 strongly inhibited endogenous Notch signaling. Immunofluorescence assay of HeLa cells exhibited that FLI-06 treatment completely disrupted Golgi but did not affect endoplasmic reticulum (ER). Microtubular cytoskeleton, mitotic spindles and the actin cytoskeleton were also preserved after FLI-06 treatment. ER export in VSVG-eGFP-transfected Hela cells was inhibited by pretreatment of 10 μM FLI-06 for 30 or 10 min. When Hela NotchE-eGFP cells pretreated with 100 μM FLI-06 for 4 hours, the budding of COPII vesicles was markedly inhibited. Incubation of 50 μM FLI-06 for 24 hours significantly upregulated the mRNA level of ngn1 in dechorionated-stage 4-hpf zebrafish embryos. Compared to control embryos, most FLI-06-treated embryos showed expanded and denser clusters of ngn1-positive cells along the spinal cord.
作用机制 FLI-06 probably inhibits Notch signaling by negatively interfering with the transport in the secretory pathway[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human MDA-MB-231 cells Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells, IC50=4 μM 26115571
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.80mL

4.56mL

2.28mL
参考文献

[1]Kramer A, Mentrup T, et al. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol. 2013 Nov;9(11):731-8.