Name: IWP-2-V2
Price: 375.00 USD

- Overview
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    Background
    
    IC50: 27 nMIWP-2-V2 is a Wnt production inhibitor.Wnt signaling proteins are small secreted proteins that are active in tissue homeostasis, embryonic development, and tumorigenesis. Wnt proteins bind to receptors, initiating a signaling cascade that results in β-catenin activation of gene transcription.In vitro: IWP-2 was identified as an inhibitor of Wnt production inactivating porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity was essential for the signaling ability and secretion of Wnt proteins. IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound. IWP-2-V2 was used to evaluate which structural features of IWP-2 were critical for impairing Wnt/β-catenin pathway activity [1].In vivo: In CCI rats, repetitive i.t. administration of IWP-2 (20 μM) in the early phase could significantly delay production of mechanical allodynia. The same drug administrated in the late phase produced long-lasting inhibitory effects on the established mechanical allodynia. Such analgesia lasted 4–6 days for IWP-2 after termination of the third treatment. These results showed similar inhibitory effects of IWP-2 on thermal hyperalgesia after CCI treatment [2].Clinical trial: So far, no clinical study has been conducted.
    
    [1] B. Chen, M. E. Dodge, W. Tang, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature Chemical Biology 5(2), 100-107 (2009).
    [2] Y. Zhang et al. WNT signaling underlies the pathogenesis of neuropathic pain in rodents. J Clin Invest. 2013 May 1; 123(5): 2268–2286.
- Properties
  - Alternative Name
    
    Inhibitor of Wnt Production-2-V2; N-(6-methyl-2-benzothiazolyl)-2-[[3,4,6,7-tetrahydro-4-oxo-3-(phenylmethyl)thieno[3,2-d]pyrimidin-2-yl]thio]-acetamide
    
    CAS Number
    
    877618-79-6
    
    Molecular Formula
    
    C23H20N4O2S
    
    Molecular Weight
    
    480.6
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤2mg/ml in DMSO;5mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

IWP-2-V2

IWP-2-V2

Background

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