Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Takinib (EDHS-206) 是一种TAK1自磷酸化的抑制剂,也是恶性疟原虫蛋白激酶 9 抑制剂,在 ATP 结合口袋内非竞争性结合。它诱导 TNF-α 刺激的细胞凋亡,可研究类风湿关节炎和转移性乳腺癌。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 597 | 现货 | ||
5 mg | ¥ 917 | 现货 | ||
10 mg | ¥ 1,224 | 现货 | ||
25 mg | ¥ 2,694 | 现货 | ||
50 mg | ¥ 3,520 | 现货 | ||
100 mg | ¥ 5,090 | 现货 | ||
200 mg | ¥ 7,230 | 现货 | ||
500 mg | ¥ 10,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 697 | 现货 |
产品描述 | Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM). |
靶点活性 | TAK1:9.5 nM |
体外活性 | Takinib reduces phosphorylation significantly but does not influence total protein levels. Takinib inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun in a dose-dependent manner. Takinib(10 mM) shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. |
激酶实验 | TAK1-TAB1 (50 ng/well) is incubated with 5 μM ATP containing radiolabeled [32P]-ATP in the presence of 300 mM substrate peptide (RLGRDKYKTLRQIRQ) in a final volume of 40 μL in the presence of buffer (containing 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% β-Mercaptoethanol, 10 mM magnesium acetate, 0.5 mM MnCl) and indicated compounds. The reaction is let go for 10 min and stopped with 10 μL concentrated H3PO4. |
细胞实验 | MDA-MB-231 cells (1,000 cells/well) are seeded in a 96-well plate with 10% FBS, 5% Pen/Strep, 4 g/L glucose DMEM medium. After 24h, cells are serum starved with 1% FBS, 5% Pen/Strep, 4 g/L glucose DMEM medium for 4h. Cells are treated with titrations of Takinib in the presence or absence of 30 ng/mL TNFα. Plates at 0 h and 24 h following treatment are frozen at -80°C after removal of media. After 24 h, 100 μL ddH2O is added to each well and plates are refrozen. 1 μL from Hoechst stock [1 mg/mL in 1:4 DMSO/H2O] is dissolved in 1 mL of TNE buffer (10 mM Tris, 2 M NaCl, 1 mM Na2EDTA) and 100 μL of this solution is added to each well. The fluorescence is determined at 355/460 nm. |
别名 | EDHS-206 |
化合物与蛋白结合的复合物 |
Crystal structure of Takinib bound to TAK1 |
分子量 | 322.36 |
分子式 | C18H18N4O2 |
CAS No. | 1111556-37-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6.8 mg/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。
Takinib 1111556-37-6 Apoptosis MAPK EDHS 206 HepG2 malaria MAP kinase kinase kinase, MEKK, MAPKKK cancer RASF Inhibitor arthritis inhibit EDHS-206 HuH7 RA-FLS EDHS206 MAP3K inhibitor