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CAS No.: 1353867-91-0

Longdaysin Catalog No. CSN24745

Synonyms: Longdaysin

Longdaysin inhibited CKIδ, CKIα, ERK2 and CDK7 with IC50 values of 8.8, 5.6, 52, and 29μM, respectively. The EC50 values of longdaysin for CKIδ and CKIα in the cell-based PER1 degradation assay were 9.7 and 9.2μM, respectively.

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生物活性

实验方案

技术信息

生物活性

描述The casein kinase I (CKI) family is a group of serine/threonine-selective enzymes that function as regulators of signaling pathways involved in circadian rhythms, DNA repair and Wnt signaling. As measured in the in vitro kinase assay, longdaysin inhibited CKIδ, CKIα, ERK2 and CDK7 with IC50 values of 8.8, 5.6, 52, and 29μM, respectively. The EC50 values of longdaysin for CKIδ and CKIα in the cell-based PER1 degradation assay were 9.7 and 9.2μM, respectively. Treatment with longdaysin (0–9μM) led to dose-dependent period lengthening in adult tail fibroblasts, lung explants, and suprachiasmatic nucleus explants from mPer2^Luc knockin mice. Longdaysin at the doses of 0.01–9μM also lengthened the period in both wild-type and CKIδ-deficient embryonic fibroblasts in a dose-dependent manner. In HEK293T cells, 10μM longdaysin reduced the CKIδ- and CKIα-dependent mobility-shift of PER1. The CKIδ- and CKIα-dependent degradation of PER1 was dose-dependently inhibited by longdaysin at the concentrations of 0-20μM. Moreover, longdaysin treatment (3 and 9µM) greatly upregulated the overall protein amount of PER1 in Bmal1-dLuc U2OS cells when compared to non-longdaysin treated controls. The administration of longdaysin (0–9μM) also resulted in >10h period lengthening in per3-luc reporter zebrafish in a dose-dependent manner^[1].
动物研究
剂量
Mice: 5 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Hirota T, Lee JW, Lewis WG, Zhang EE, Breton G, Liu X, Garcia M, Peters EC, Etchegaray JP, Traver D, Schultz PG, Kay SA. High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase. PLoS Biol. 2010 Dec 14;8(12):e1000559.

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
- 2.9822 mL
- 14.9108 mL
- 29.8216 mL
- 5 mM
- 0.5964 mL
- 2.9822 mL
- 5.9643 mL
- 10 mM
- 0.2982 mL
- 1.4911 mL
- 2.9822 mL

技术信息

CAS号

1353867-91-0

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

C16H16F3N5

运输

蓝冰

分子量

335.33

别名

Longdaysin

溶解度

DMSO	25.5 mg/mL (76.0 mM)
Water	insoluble

动物实验配方

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