IWP-2-V2

An inhibitor of Wnt production

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货号: ajci13334
CAS: 877618-79-6
别名: Inhibitor of Wnt Production-2-V2
分子式: C23H20N4O2S
分子量: 480.6
纯度: >98%
溶解度: ≤2mg/ml in DMSO;5mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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.

参考文献:
[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.