Longdaysin
产品说明书
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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： |
Pure form Keep in dark place,Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 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 | |||
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| 1mg | 5mg | 10mg | |
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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 |
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