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IWP-2-V2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IWP-2-V2图片
CAS NO:877618-79-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Cas No.877618-79-6
别名Inhibitor of Wnt Production-2-V2
化学名N-(6-methyl-2-benzothiazolyl)-2-[[3,4,6,7-tetrahydro-4-oxo-3-(phenylmethyl)thieno[3,2-d]pyrimidin-2-yl]thio]-acetamide
Canonical SMILESO=C(CSC(N1CC2=CC=CC=C2)=NC3=C(SCC3)C1=O)NC4=NC5=C(C=C(C)C=C5)S4
分子式C23H20N4O2S
分子量480.6
溶解度≤2mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.