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Longdaysin

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Chemical Structure| 1353867-91-0 同义名 : -
CAS号 : 1353867-91-0
货号 : A1177302
分子式 : C16H16F3N5
纯度 : 99%+
分子量 : 335.327
MDL号 : MFCD20527323
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: 120 mg/mL(357.86 mM),配合低频超声助溶,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
靶点
  • CK1

    CKIδ, IC50:8.8 μM

    CKIα, IC50:5.6 μM

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 mPer2Luc 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.91mL

2.98mL

1.49mL

29.82mL

5.96mL

2.98mL

参考文献

[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.