Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (298.21 mM)
H2O: Insoluble
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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