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CAS No.: 313967-18-9

FLI-06 Catalog No. CSN18205

Synonyms: FLI-06

FLI-06 is a Notch signaling inhibitor with EC50 of 2.3 μM which can disrupt Notch trafficking and processing.

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生物活性

实验方案

技术信息

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
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
human MDA-MB-231 cells - Cytotoxicity assay - Cytotoxicity against human MDA-MB-231 cells, IC50=4 μM 26115571
动物研究
剂量
Mice: 1 mg/kg^[2] (i.p.), 40 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human MDA-MB-231 cells	-	Cytotoxicity assay	-	Cytotoxicity against human MDA-MB-231 cells, IC50=4 μM	26115571

动物研究
剂量	Mice: 1 mg/kg^[2] (i.p.), 40 mg/kg^[3] (i.p.)
给药途径	i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2804 mL
- 11.4020 mL
- 22.8040 mL
- 5 mM
- 0.4561 mL
- 2.2804 mL
- 4.5608 mL
- 10 mM
- 0.2280 mL
- 1.1402 mL
- 2.2804 mL

技术信息

CAS号

313967-18-9

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H30N2O5

运输

蓝冰

分子量

438.52

别名

FLI-06

溶解度

DMSO	87.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	8.0 mg/mL (18.2 mM)

动物实验配方

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