AG-18
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.
AG18是EGFR激酶的抑制剂，IC50值为35 μM[3]。
AG18是酪氨酸激酶的抑制剂，阻断酪氨酸的磷酸化及其下游事件[1]。
在缺乏毒蕈碱受体激动剂氨甲酰胆碱的情况下，AG18和AG10减少了90％的细胞内ATP，增加了氧消耗率，这表明这些酪氨酸磷酸化抑制剂不与线粒体耦合。仅在降低ATP含量的浓度下，AG18和AG10阻断腮腺的磷酸化事件。在HEK293、PC12和HeLa细胞中，AG18和AG10也激活AMPK，不耦合线粒体[1]。
在粒黄体细胞中，酪氨酸磷酸化抑制剂AG18可逆地阻止FSH诱导的P450scc mRNA积累，IC50值为15 μM，然而，AG18不能加速mRNA的降解过程。此外，在培养基中加入AG18并没有影响粒黄体细胞中极高水平的P450scc mRNA。AG18抑制芳香化酶细胞色素P450和3β-羟基脱氢酶-I的mRNA含量[2]。
参考文献：
[1]. Soltoff SP. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling. J Biol Chem. 2004 Mar 19;279(12):10910-8. Epub 2003 Dec 19.
[2]. Orly J, Rei Z, Greenberg NM et al. Tyrosine kinase inhibitor AG18 arrests follicle-stimulating hormone-induced granulosa cell differentiation: use of reverse transcriptase-polymerase chain reaction assay for multiple messenger ribonucleic acids. Endocrinology. 1994 Jun;134(6):2336-46.
[3]. Gazit A, Yaish P, Gilon C et al. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem. 1989 Oct;32(10):2344-52.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 186.17 |
| Cas No. | 118409-57-7 |
| Formula | C10H6N2O2 |
| Solubility | insoluble in H2O; ≥15 mg/mL in EtOH; ≥9.3 mg/mL in DMSO |
| Chemical Name | 2-[(3,4-dihydroxyphenyl)methylidene]propanedinitrile |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=C(C=C1C=C(C#N)C#N)O)O |
| 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 | AG-18 is an inhibitor of epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR) kinase with IC50 values of 35 µM and 25 μM, respectively. | |||||
| Targets | EGFR | PDGFR | ||||
| IC50 | 35 µM | 25 μM | ||||
质量控制和MSDS
- 批次:
化学结构
