Decanoyl-RVKR-CMK

Decanoyl-RVKR-CMK

Catalog Number:
L002371009APE
Mfr. No.:
APE-B5437
Price:
$266
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative 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
          CAS Number
          150113-99-8
          Molecular Formula
          C34H66ClN11O5
          Molecular Weight
          744.42
          Appearance
          A crystalline solid
          Purity
          Purity ≥95.00%
          Solubility
          Soluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Xiaoman Liu, Liang Wei, et al. "SARS-CoV-2 spike protein–induced cell fusion activates the cGAS-STING pathway and the interferon response." Sci Signal. 2022 Apr 12;15(729):eabg8744. PMID: 35412852
          2. David Zaragoza-Huesca, Carlos Martínez-Cortés, et al. "Identification of Kukoamine A, Zeaxanthin, and Clexane as New Furin Inhibitors." Int J Mol Sci. 2022 Mar 3;23(5):2796. PMID: 35269938

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