IWP-2

基本信息

分子式	C22H18N4O2S3
分子量	466.60
存储条件	Freezer -20℃

半岛bd体育手机客户端 描述

IWP-2是一种Wnt信号和分泌抑制剂，无细胞试验中IC50为27 nM，选择性阻断Porcn介导的Wnt棕榈酰化，一般不影响Wnt/β-catenin，且对Wnt刺激的细胞反应没有影响

靶点（IC50 & Targe）

Wnt,27nM

Selective inhibitor of Porcn-mediated Wnt secretion.

体外研究

IWP-2在再生医学和抗癌方面都非常有效。IWP-2使Porcn失活, Porcn是一种与O-酰基转移酶(MBOAT)结合的膜,且选择性抑制Wnt棕榈酰化。IWP-2抑制Lrp6受体和Dvl2发生Wnt依赖性的磷酸化，也抑制β-catenin累积。[1]

细胞实验

Cell lines: L-Wnt-STF cells

Concentrations: 5 μM

Incubation Time: 24 h

Method: L-Wnt-STF cells that exhibit constitutive Wnt pathway activation were incubated with IWR (10μM) and IWP (5μM) compounds for 24 hrs prior to lysis. Cellular lysates were subjected to Western blot analysis.

(Only for Reference)

动物实验

Animal Models: Crl:CD1 (ICR) and FVB/N female mice

Formulation: encapsulated in liposomes

Dosages: 50 ?g

Administration: s.c.

(Only for Reference)

参考文献

[1] Chen B, et al. Nat Chem Biol, 2009, 5(2), 100-107.

[2] Castellana D, et al. PLoS Biol. 2014, 12(12):e1002002.