IWP-2 是一种 Wnt 加工和分泌抑制剂，IC50为 27 nM。它还是一种具有 ATP 竞争能力的CK1δ抑制剂，对于M82FCK1δ的IC50为 40 nM。在无细胞试验中，它可选择性阻断 Porcn 介导的 Wnt 棕榈酰化。

IWP-2, an inhibitor of Wnt processing and secretion (IC50=27 nM) in a cell-free assay, selectively blocks Porcn-mediated Wnt palmitoylation.

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[3]. Pretreatment with IWP-2 significantly (P<0.05) abolished SP-induced increase of Wnt3a, p-GSK3β, and β-catenin expressions[4].

IWP-2 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. The human RCC cell lines 786O and Caki-2 (5×103) are seeded into 96-well plates. Cell viability is estimated by MST assay after Caki-2 acells are incubated with ncreasing concentrations of LEF together with 20 μM IWP-2 for 48 h.After treatment, 10 μL MTS is added into each well for 2 h incubation. The absorbance is measured using a model ELX800 Micro Plate Reader at 490 nm. For colony formation assay, Caki-2 cells are trypsinized to single cell suspensions and seeded into fresh 6-well plates at 1000 cells/well. Then cells are incubated with LEF at depicted concentrations for 7 days. Colonies are fixed with absolute methanol for 15 min and then stained with 0.1% crystal violet for 20 min. After washing with PBS three times, the colonies with a diameter over 2 mm are visualized by a digital camera[2].

686770-61-6

C22H18N4O2S3

466.59

IWP2

DMSO:2mg/ml（4.29mM）
Powder: -20°C for 3 years
In solvent: -80°C for 2 years