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- 技术资料
- CAS号：
522629-08-9
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥234.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥551.0 |
| 规格： | 5mg | 产品价格： | ￥510.0 |
| 规格： | 10mg | 产品价格： | ￥789.0 |
| 规格： | 25mg | 产品价格： | ￥1584.0 |
| 规格： | 50mg | 产品价格： | ￥2544.0 |
| 规格： | 100mg | 产品价格： | ￥3672.0 |
Product Introduction
Bioactivity
| 名称 | CGP 57380 |
| 描述 | CGP 57380 (MNK1 Inhibitor) is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. |
| 激酶实验 | Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors. |
| 体外活性 | CGP57380 以约 3 μM 的 IC50 在体外抑制 eIF4E 的磷酸化。CGP57380 导致 eIF4E 脱磷酸化，并在 293 细胞中进一步增加帽依赖性报告。[1] CGP57380 导致剂量依赖性减少 Ang II 激活的 eIF4E 磷酸化、蛋白质合成和 VSMC 肥大。[2] CGP57380 使野生型细胞对小鼠胚胎成纤维细胞 (MEFs) 中血清撤离诱导的凋亡更加敏感。[3] CGP57380 阻止 BC 祖细胞的连续重复培养功能。[4] |
| 体内活性 | CGP57380（40 mg/kg/d i.p.）有效地消除了BC CML细胞连续移植免疫缺陷小鼠以及作为LSCs的能力。[4] |
| 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 | 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 : 2 mg/mL (8.19 mM), Sonication is recommended. DMSO : 45 mg/mL (184.25 mM), Sonication is recommended. |
| 关键字 | MNK2 | MNK1 | MNK | Mitogen activated protein kinase interacting kinase | MAPK interacting kinase | MAP kinase interacting kinase | Inhibitor | inhibit | CGP-57380 | CGP57380 | CGP 57380 | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Colorectal Cancer Compound Library | Kinase Inhibitor Library | Anti-Fibrosis Compound Library | Highly Selective Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Pain-Related Compound Library | Target-Focused Phenotypic Screening Library |
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化合物 CGP 57380【522629-08-9】
￥234 - 3672
