| CAS NO: | 122520-90-5 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 268.2 |
| Cas No. | 122520-90-5 |
| Formula | C13H8N4O3 |
| Synonyms | Tyrphostin 51 |
| Solubility | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | 2-amino-4-(3,4,5-trihydroxyphenyl)-1,3-butadiene-1,1,3-tricarbonitrile |
| Canonical SMILES | OC1=C(O)C(O)=CC(/C=C(C#N)/C(N)=C(C#N)\C#N)=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
AG-183, a member of tyrphostin, is an inhibitor of protein tyrosine kinase [1].
Protein tyrosine kinase is an enzyme that catalyzes the transfer of the γ phosphate of ATP to tyrosine residues on protein substrates. Phosphorylation of proteins by kinases is an important mechanism in signal transduction and regulating cellular activity, such as cell division. Tyrosine phosphorylation is a key covalent modification that occurs in multicellular organisms as a result of intercellular communication during embryogenesis and maintenance of adult tissues. Phosphorylation of tyrosine residues modulates enzymatic activity and creates binding sites for the recruitment of downstream signaling proteins [2].
PTK inhibitors could preferentially inhibit the epidermal growth factor (EGF) receptor kinase to block EGF-dependent cell proliferation [1]. In the human epidermoid carcinoma cell line, A431AG-183 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 800 nM [1].
References:
[1] Gazit A, Yaish P, Gilon C, et al. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors[J]. Journal of medicinal chemistry, 1989, 32(10): 2344-2352.
[2] Hubbard S R, Till J H. Protein tyrosine kinase structure and function[J]. Annual review of biochemistry, 2000, 69(1): 373-398.
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