CGP 57380
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CGP 57380是特异的和选择性的MNK1抑制剂,IC50值为2.2 μM[1].
有丝分裂原激活蛋白(MAP)激酶相互作用激酶1(MNK1)是丝氨酸/苏氨酸激酶,能够整合来自MAP激酶信号通路的信号,磷酸化eIF4E [1].
CGP 57380是特异的和选择性的MNK1抑制剂.在293细胞中,CGP 57380 (10 μM)抑制响应于胎牛血清(FCS)\亚硝酸盐\茴香霉素\PMA或肿瘤坏死因子α的eIF4E磷酸化.CGP 57380也能提高cap依赖的报告基因rluc.在细胞实验中,CGP 57380抑制eIF4E磷酸化,IC50值为3 μM [1].在大鼠血管平滑肌细胞中,CGP 57380以剂量依赖的方式抑制血管紧张素II诱导的eIF4E磷酸化\蛋白合成和VSMC肥大[2].在小鼠巨噬细胞中,CGP 57380通过转录后调控,浓度依赖性地抑制由大肠杆菌脂多糖(LPS)刺激的TNF-α产生.CGP 57380也能抑制eIF4E磷酸化.这些结果表明包含腺嘌呤/尿苷富集原件(ARE)的TNF-α mRNA需要eIF4E磷酸化以起始翻译[3].在骨髓衍生的巨噬细胞中,CGP 57380显著抑制促炎细胞因子单核细胞趋化蛋白-1\TNF和IL-6的产生[4].
参考文献：
[1]. Knauf U, Tschopp C, Gram H. Negative regulation of protein translation by mitogenactivated protein kinase-interacting kinases 1 and 2. Mol Cell Biol, 2001, 21(16): 5500-5511.
[2]. Ishida M, Ishida T, Nakashima H, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res, 2003, 93(12): 1218-1224.
[3]. Andersson K, Sundler R. Posttranscriptional regulation of TNFalpha expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine, 2006, 33(1): 52-57.
[4]. Rowlett RM, Chrestensen CA, Nyce M, et al. MNK kinases regulate multiple TLR pathways and innate proinflammatory cytokines in macrophages. Am J Physiol Gastrointest Liver Physiol, 2008, 294(2): G452-459.
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 244.23 |
| Cas No. | 522629-08-9 |
| Formula | C11H9FN6 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥12.2 mg/mL in DMSO |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=C(C=C1)NC2=NNC3=C2C(N)=NC=N3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | CGP 57380是高效的MNK1抑制剂,IC50值为2.2 μM. | |||||
| 靶点 | MNK1 | |||||
| IC50 | 2.2 μM | |||||
