| CAS NO: | 150113-99-8 |
| 包装 | 价格(元) |
| 500ug | 电议 |
| 1mg | 电议 |
| 5mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 744.42 |
| Cas No. | 150113-99-8 |
| Formula | C34H66ClN11O5 |
| Solubility | Soluble in H2O |
| Chemical Name | (2S,5R,8R,11S)-5-(4-aminobutyl)-2,11-bis(3-((diaminomethylene)amino)propyl)-8-isopropyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazatricosan-1-oyl chloride |
| Canonical SMILES | ClC([C@H](CCC/N=C(N)\N)NC([C@@H](CCCCN)NC([C@@H](C(C)C)NC([C@H](CCC/N=C(N)\N)NC(CCCCCCCCCC)=O)=O)=O)=O)=O |
| 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。 |
Decanoyl-RVKR-CMK is a proprotein convertase inhibitor [1].
Proprotein convertases (PCs) are involved in generating bioactive peptides, as well as activating several enzymes and growth factors in many important physiological events. PCs play important roles in several pathologies including viral infections and cancers. Thus, PCs are promising targets for therapeutic applications [1].
In PC12 cells, the PC enzyme inhibitor decanoyl-RVKR-CMK at ~ 100 μM, resulted in partial block of regulated VGF release at 48 h and a complete block at 96 h, without significant change in basal VGF release. Also, decreased VGF processing was observed in cell extracts and media from decanoyl-RVKR-CMK-treated PC12 cultures [2].
In K5-PACE4 transgenic mice topically treated with the hyperplasiogenic phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA), a 2-day topical treatment of decanoyl-RVKR-CMK at 300 μM, inhibited TPA-induced epidermal proliferation. When decanoyl-RVKR-CMK treatment (100 μM, q.d.) was extended for 3 weeks, decreasing numbers of Ki-67-labeled cells were shown in both K5-PACE4 mice epidermal basal epidermal keratinocytes and wild-type mouse epidermis [3].
References:
[1]. Fugère M, Day R. Cutting back on pro-protein convertases: the latest approaches to pharmacological inhibition. Trends in Pharmacological Sciences, 2005, 26(6): 294-301.
[2]. Garcia A L, Han S K, Janssen W G, et al. A prohormone convertase cleavage site within a predicted alpha-helix mediates sorting of the neuronal and endocrine polypeptide VGF into the regulated secretory pathway. Journal of Biological Chemistry, 2005, 280(50): 41595-41608.
[3]. Bassi D E, Zhang J, Cenna J, et al. Proprotein convertase inhibition results in decreased skin cell proliferation, tumorigenesis, and metastasis. Neoplasia, 2010, 12(7): 516-526.
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