IWP-2-V2 (Synonyms: Inhibitor of Wnt Production-2-V2) |
Catalog No.GC14546 |
Wnt production inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 877618-79-6
Sample solution is provided at 25 µL, 10mM.
IC50: 27 nM
IWP-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.
References:
[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.
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