Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RKI-1447 是一种高效的ROCK1和ROCK2的小分子抑制剂,IC50值分别为14.5和6.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 487 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,990 | 现货 | ||
50 mg | ¥ 2,780 | 现货 | ||
100 mg | ¥ 3,650 | 现货 | ||
200 mg | ¥ 5,270 | 现货 | ||
500 mg | ¥ 8,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities. |
靶点活性 | ROCK1:14.5 nM, ROCK2:6.2 nM |
体外活性 | RKI-1447抑制87%乳腺肿瘤的生长,并且和对照小鼠相比,乳腺肿瘤平均体积减小7.7倍.RKI-1447在转基因小鼠模型中,有效抑制乳腺肿瘤的生长.小鼠肿瘤用RKI-1447处理时,肿瘤体积增加的平均百分比仅为8.8%. |
体内活性 | RKI-1447抑制人癌细胞中ROCK底物MLC-2和MYPT-1的磷酸化,但对浓度高达10 μM的AKT,MEK和S6激酶的磷酸化水平没有影响。RKI-1447抑制乳腺癌细胞的迁移,侵袭和锚定非依赖性肿瘤的生长。RKI-1447/ROCK1复合物的晶体结构显示RKI-1447是I型激酶抑制剂,其通过与铰链区和DFG基序的相互作用结合ATP结合位点。 |
激酶实验 | Z-Lyte FRET kinase assay: Kinase inhibition is measured using the Invitrogen Z-Lyte? FRET kinase assay with Ser/Thr 13 peptide substrate based on the myosin light chain sequence KKRPQRRYSNVF. Compounds are tested on three separate days with 8 point dilutions performed in duplicate to determine average IC50 values. The assay conditions are optimized to 15 μL of kinase reaction volume with 5 ng of enzyme in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, and 0.01% Brij-35. The reaction is incubated for 1 h at room temperature in the presence of 1.5 μM of peptide substrate with 12.5 μM of ATP (for ROCK1) or 2 μM of substrate with 50 μM of ATP (for ROCK2). The reaction is then stopped and the ratio of phosphorylated to unphosphorylated peptides is determined by selective cleavage of only the unphosphorylated peptide as described by the manufacturer. This is followed by excitation of coumarin at 400 nm resulting in emission at 445 nm and energy transfer to fluorescein and final emission at 520 nm. The substrate contains both coumarin and fluorescein and only uncleaved phosphorylated substrate will undergo FRET. The ratio of the signals at 445 nm and 520 nm is measured using a Wallac EnVision Plate Reader, model 2102 plate-reader. |
细胞实验 | Cells are plated in a 96 well tissue culture plate (1200 cells per well) and incubated for 24 hours. After incubation the cells are treated with vehicle or increasing concentrations of RKI-1447 for 72 hours. After incubation, freshly prepared MTT (2 mg/ml) is added to each well and incubated for 3 hours. After incubation the plates are read at 540 nm. (Only for Reference) |
别名 | RKI1447 |
分子量 | 326.37 |
分子式 | C16H14N4O2S |
CAS No. | 1342278-01-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 18.33 mg/mL (56.17 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.064 mL | 15.32 mL | 30.6401 mL | 76.6002 mL |
5 mM | 0.6128 mL | 3.064 mL | 6.128 mL | 15.32 mL | |
10 mM | 0.3064 mL | 1.532 mL | 3.064 mL | 7.66 mL | |
20 mM | 0.1532 mL | 0.766 mL | 1.532 mL | 3.83 mL | |
50 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.532 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。
RKI-1447 1342278-01-6 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK Rho-kinase Inhibitor inhibit ROK Rho-associated kinase RKI1447 Rho-associated protein kinase RKI 1447 inhibitor