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- CAS号：
1342278-01-6
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥188.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥436.0 |
| 规格： | 5mg | 产品价格： | ￥389.0 |
| 规格： | 10mg | 产品价格： | ￥662.0 |
| 规格： | 25mg | 产品价格： | ￥1320.0 |
| 规格： | 50mg | 产品价格： | ￥2120.0 |
| 规格： | 100mg | 产品价格： | ￥2920.0 |
| 规格： | 200mg | 产品价格： | ￥4216.0 |
Product Introduction
Bioactivity
| 名称 | RKI-1447 |
| 描述 | RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities. |
| 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) |
| 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. |
| 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。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 10 mg/mL (30.64 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 122.5 mg/mL (375.34 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (30.64 mM), Solution. |
| 关键字 | ROK | ROCK2 | ROCK1 | ROCK | RKI-1447 | RKI 1447 | Rho-kinase | Rho-associated protein kinase | Rho-associated kinase | Inhibitor | inhibit |
| 相关产品 | Y-27632 dihydrochloride | ITX3 | CID-5056270 | Fasudil hydrochloride | ROCK-IN-5 | Fasudil | Tofacitinib | CAY10746 | Y-27632 | SAR407899 hydrochloride | Thiazovivin | GSK180736A |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Neural Regeneration Compound Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | TGF-beta/Smad Compound Library | Membrane Protein-targeted Compound Library | Anti-Metabolism Disease Compound Library | Target-Focused Phenotypic Screening Library |
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相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 RKI-1447【1342278-01-6】
￥188 - 4216
