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Longdaysin

Longdaysin

产品编号 T5358   CAS 1353867-91-0

Longdaysin 是一种 CK1α 和 CK1δ 的抑制剂,IC50为5.6和8.8 µM。它还抑制ERK2,IC50值为52 µM。它是Wnt/β-catenin 信号通路的抑制剂,通过阻断CK1δ/ε依赖性 Wnt 信号通路发挥抗肿瘤作用。

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Longdaysin Chemical Structure
Longdaysin, CAS 1353867-91-0
规格 价格/CNY 货期 数量
1 mg ¥ 295 现货
5 mg ¥ 747 现货
10 mg ¥ 1,190 现货
25 mg ¥ 2,390 现货
50 mg ¥ 3,820 现货
100 mg ¥ 5,550 现货
1 mL * 10 mM (in DMSO) ¥ 822 现货
产品目录号及名称: Longdaysin (T5358)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6/8.8 μM). It also can inhibit ERK2 (IC50: 52 μM).
靶点活性 CDK7:29 μM (cell free), ERK2:52 μM (cell free), CKIα:5.6 μM (cell free), CKIδ:8.8 μM (cell free)
体外活性 Longdaysin inhibited CKIδ, CKIα, ERK2, and CDK7 activities (IC50?=?8.8, 5.6, 52, and 29 μM, respectively), while it had much less effect on p38α. The period of CKIδ deficient cells was 1.1 h longer than that of wild type cells. Longdaysin lengthened the period in a dose-dependent manner in CKIδ deficient cells as well as in wild type cells [1]. In breast cancer Hs578T and MDA-MB-231 cells, micromolar concentrations of longdaysin attenuated the phosphorylation of LRP6 and DVL2 and reduced the expression of active β-catenin and total β-catenin, leading to the downregulation of Wnt target genes Axin2, DKK1, LEF1, and Survivin [2].
体内活性 In MDA-MB-231 breast cancer xenografts, treatment with longdaysin suppressed tumor growth in association with inhibition of Wnt/β-catenin signaling [2].
激酶实验 The CKIδ, CKIα, CDK7, and ERK2 kinase assays were performed on 384-well plates (10 μl volume). The reaction mixture was as follows: for CKIδ, 2 ng/μl CKIδ, 50 μM peptide substrate RKKKAEpSVASLTSQCSYSS corresponding to human PER2 Lys659-Ser674, and CKI buffer (40 mM Tris, 10 mM MgCl2, 0.5 mM DTT, 0.1 mg/ml BSA, pH 7.5); for CKIα, 1 ng/μl CKIα, 50 μM CKI peptide substrate, and CKI buffer; for CDK7, 5 ng/μl CDK7, 100 μM Cdk7/9 peptide substrate, and CKI buffer; for ERK2, 1.5 ng/μl ERK2, 0.8 μg/μl MBP, and ERK buffer (50 mM Tris, 10 mM MgCl2, 0.5 mM DTT, 1 mM EGTA, pH 7.5). Five hundred nl of compound was added to the mixture (final 5% DMSO), and the reaction was started by adding ATP (final 5 μM). After incubation at 30°C for 3h, 10 μl of Kinase-Glo Luminescent Kinase Assay reagent was added, and the luminescence was detected to determine the remaining ATP amount. All of the tested compounds did not inhibit luciferase activity directly [1].
细胞实验 2×10^5 cells were suspended in 100 μL serum-free medium containing the indicated concentrations of longdaysin, and then seeded in 24-transwell chambers with 8 μm pore membrane. The lower chamber contained medium with 20% FBS. After incubation at 37°C for 6 hours, the unmigrated cells on the upper side of membrane were removed by a cotton swab, and the migrated cells were stained with crystal violet and stained cells were photomicrographed. For invasion assays, the transwell chambers with 8 μm pore membranes were coated with Matrigel [2].
动物实验 MDA-MB-231 cells were injected s.c. into the right flank of nude mice (1×10^7 cells per mouse), and tumor growth was closely observed and measured every 3 days. When the tumors reached approximately 50 mm3, the mice were randomly divided into two groups (eight mice per group) and i.p. injected with the vehicle (0.8% DMSO/12% Cremophor/8% ethanol in normal saline) or 5 mg/kg longdaysin in vehicle every 3 days. This longdaysin dosage was selected based on results from preliminary experiments, and was well tolerated in the mouse model. Subsequently, tumor volumes were measured with a caliper and calculated as follows: 0.523×(length)×(width)2. After treatment for 3 weeks, the mice were sacrificed and the tumor tissues were collected and weighed before being fixed in buffered formalin [2].
分子量 335.33
分子式 C16H16F3N5
CAS No. 1353867-91-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (298.21 mM)

H2O: Insoluble

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9821 mL 14.9107 mL 29.8214 mL 74.5534 mL
5 mM 0.5964 mL 2.9821 mL 5.9643 mL 14.9107 mL
10 mM 0.2982 mL 1.4911 mL 2.9821 mL 7.4553 mL
20 mM 0.1491 mL 0.7455 mL 1.4911 mL 3.7277 mL
50 mM 0.0596 mL 0.2982 mL 0.5964 mL 1.4911 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7455 mL

计算器

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分子量计算器
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参考文献

1. Hirota T, et al. 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. 2. Xiong Y, et al. Longdaysin inhibits Wnt/β-catenin signaling and exhibits antitumor activity against breast cancer. Onco Targets Ther. 2019 Feb 5;12:993-1005.
Fadraciclib Lerociclib Kobophenol A Aloisine B CDK-IN-10 THZ2 InhA-IN-2 BX-912

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 HIF-1化合物库 抗乳腺癌化合物库 代谢化合物库 抗前列腺癌化合物库 经典已知活性库 癌细胞分化化合物库 谷氨酰胺代谢化合物库 抗衰老化合物库 抗结直肠癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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g
给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Longdaysin 1353867-91-0 Cell Cycle/Checkpoint MAPK Metabolism Stem Cells ERK Casein Kinase CDK Cyclin dependent kinase inhibit Inhibitor Extracellular signal regulated kinases inhibitor

 

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