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 NotchE-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].
FLI-06 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
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