"目录号: HY-13912
Stem Cell/Wnt-
IWP-2 抑制Wnt加工和分泌，IC50为 27 nM。
Wnt
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生物活性
Description
IWP-2 is an inhibitor ofWntprocessing and secretion withIC50of 27 nM.
IC50& Target
IC50: 27 nM (Wnt)[1]
In Vitro
IWP-2, an inhibitor of WNT processing and secretion. IWP-2 significantly enhances the anti-proliferative effect of LEF. It is also obvious that the combination of LEF and IWP-2 could minimize the expression of β-catenin, c-Myc, Cyclin D1, Bcl2 and Bax to the largest extent compared with single agents[2]. Following treatment in the MKN28 cell line for four days, 10-50 μM IWP-2 significantly suppressed the proliferation of MKN28 cells (P<0.05). In addition, anchor-dependent and anchor-independent colony numbers are significantly decreased following IWP-2 treatment (P<0.05)[3].
In Vivo
To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the anti-inflammatory cytokine IL-10[4]. Pretreatment with IWP-2 significantly (P<0.05) abolished SP-induced increase of Wnt3a, p-GSK3β, and β-catenin expressions[5].
References
[1].Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.
[2].Chen Y, et al. Inhibition of canonical WNT/β-catenin signaling is involved in leflunomide (LEF)-mediated cytotoxic effects on renal carcinoma cells. Oncotarget. 2016 Jul 6.
[3].Mo ML, et al. Inhibition of the Wnt palmitoyltransferase porcupine suppresses cell growth and downregulates the Wnt/β-catenin pathway in gastric cancer. Oncol Lett. 2013 May;5(5):1719-1723.
[4].Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5.
[5].Liu JD, et al. Wnt/Glycogen Synthase Kinase 3β/β-catenin Signaling Activation Mediated Sevoflurane Preconditioning-induced Cardioprotection. Chin Med J (Engl). 2015 Sep 5;128(17):2346-53.