DEL-22379
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.
DEL-22379是ERK二聚化的抑制剂,对致癌细胞基因型的IC50值范围为150-400 nM[1]。
作为ERK信号的空间调节器,ERK二聚化是必不可少的。阻碍ERK的二聚化导致ERK信号核外成分障碍,从而减弱肿瘤发展和细胞转化[1]。
在HEK293细胞中,DEL-22379消除了EGF刺激的ERK二聚化。在这些细胞中,DEL-22379消除了EGF诱导的免疫共沉淀和血球凝集素或FLAG标记的异位ERK2分子,IC50值大约为0.5 μM。在这两个实验中,DEL-22379对ERK二聚的抑制与ERK磷酸化无关。在EGF刺激的HeLa细胞的细胞质中,ERK二聚化十分明显,但在DEL-22379预处理下没有检测到ERK二聚体[1]。
在一些肿瘤细胞系异种移植的裸鼠中,剂量15 mg/kg的DEL-22379抑制了异种移植肿瘤和肝脏提取物中ERK的二聚化。DEL-22379显著地抑制了A375细胞(BRAF突变体)的肿瘤进展。激活的RAS驱动肿瘤对DEL-22379非常敏感。数据显示,ERK二聚化对肿瘤增殖至关重要。在肿瘤中,DEL-22379治疗引起了广泛粘液分化和细胞死亡[1]。
参考文献:
[1]. Herrero A, Pinto A, Colón-Bolea P, et al. Small molecule inhibition of ERK dimerization prevents tumorigenesis by RAS-ERK pathway oncogenes. Cancer cell, 2015, 28(2): 170-182.
Storage | Store at -20°C |
M.Wt | 444.53 |
Cas No. | 181223-80-3 |
Formula | C26H28N4O3 |
Solubility | Soluble in DMSO |
Chemical Name | N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide |
SDF | Download SDF |
Canonical SMILES | O=C1NC2=CC=C(NC(CCN3CCCCC3)=O)C=C2C1=CC4=CNC5=CC=C(OC)C=C54 |
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。 |