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货期:1-2天
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MedChemExpress LLC
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5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 5 mg | 产品价格: | ¥500.0 |
|---|---|---|---|
| 规格: | 10 mg | 产品价格: | ¥800.0 |
| 规格: | 25 mg | 产品价格: | ¥1600.0 |
| 规格: | 50 mg | 产品价格: | ¥2600.0 |
| 规格: | 100 mg | 产品价格: | ¥4100.0 |
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IWP-2
CAS No. : 686770-61-6
MCE 国际站:IWP-2
产品活性:IWP-2 是 Wnt 加工和分泌的抑制剂,其 IC50 为 27 nM。IWP-2 靶向膜结合的 O-酰基转移酶 porcupine (Porcn),从而阻止关键的 Wnt 配体棕榈糖基化。IWP-2 还是一种具有 ATP 竞争能力的 CK1δ 抑制剂,对于 M82FCK1δ 的 IC50 为 40 nM。
研究领域:Stem Cell/Wnt | Cell Cycle/DNA Damage
作用靶点:Wnt | Porcupine | Casein Kinase
In Vitro: IWP-2 inhibits the proliferation of the investigated cell lines within the single digit μM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC50s of 8.96 μM, 1.90 μM, 2.33 μM, 3.86 μM, 4.67 μM, 2.76 μM, 1.90 μM and 2.05 μM, respectively.
Panc-1 cells are either untreated or treated with 2.33 μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells.
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.
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