Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of SIK substrate CRTC3 at S370. MRT199665 induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 8-10周 | ||
50 mg | ¥ 13,800 | 8-10周 | ||
100 mg | ¥ 17,500 | 8-10周 |
产品描述 | MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of SIK substrate CRTC3 at S370. MRT199665 induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells. |
靶点活性 | MELK:29 nM, AMPK α2:10 nM, TBK1:5400 nM, SIK1:110 nM, BRSK2:10000 nM, MARK4:2 nM, IKKε:7700 nM, SIK2:12 nM, SIK3:43 nM, MARK3:3 nM, NUAK1:3 nM, NUAK2:120 nM, MARK1:2 nM, MARK2:2 nM, AMPK α1:10 nM |
体外活性 | MRT199665 also causes a decrease in total MEF2C protein. MRT199665 (1 μM; pre-treated for 1 h) enhances LPS (100 ng/mL; stimulated for up to 24 h)-stimulated IL-10 mRNA and Nurr77 mRNA production, and IL-10 secretion. MRT199665 treatment can block MEF2C S222 phosphorylation in acute myeloid leukemia (AML) cells. MRT199665 (1 nM-100 μM; 48 hours) decreases leukemia growth. MRT199665 (10 nM-1000 nM; 12 hours) leads to a dose-dependent reduction in total and pS222 MEF2C [1][2]. |
分子量 | 469.58 |
分子式 | C28H31N5O2 |
CAS No. | 1456858-57-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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