Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HTH-01-015 是一种选择性 NUAK1 抑制剂,IC50为 100 nM。它抑制 NUAK1 的效力比抑制 NUAK2 高 100 倍以上,IC50大于10 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 269 | 现货 | ||
2 mg | ¥ 382 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 996 | 现货 | ||
25 mg | ¥ 1,780 | 现货 | ||
50 mg | ¥ 2,990 | 现货 | ||
100 mg | ¥ 3,950 | 现货 | ||
500 mg | ¥ 8,560 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 688 | 现货 |
产品描述 | HTH-01-015 is a selective NUAK1 inhibitor (IC50=100 nM). |
靶点活性 | NUAK1:100 nM |
体外活性 | In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. HTH-01-015 suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, HTH-01-015 inhibits cell proliferation in both cell lines. [1] HTH-01-015 inhibitors markedly restricted cells from entering into mitosis in U2OS cells. [2] |
激酶实验 | Kinase activity assays: In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h. |
细胞实验 | Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96? AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015.(Only for Reference) |
分子量 | 468.55 |
分子式 | C26H28N8O |
CAS No. | 1613724-42-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 54 mg/mL (115.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 28 mg/mL (59.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1342 mL | 10.6712 mL | 21.3424 mL | 53.3561 mL |
5 mM | 0.4268 mL | 2.1342 mL | 4.2685 mL | 10.6712 mL | |
10 mM | 0.2134 mL | 1.0671 mL | 2.1342 mL | 5.3356 mL | |
20 mM | 0.1067 mL | 0.5336 mL | 1.0671 mL | 2.6678 mL | |
50 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0671 mL | |
DMSO | 100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5336 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。
HTH-01-015 1613724-42-7 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK inhibit AMP-activated protein kinase HTH 01 015 HTH01015 Inhibitor inhibitor