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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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Cytoskeleton Compound Library | Neuroprotective Compound Library | Anti-Breast Cancer Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | CK2-IN-4 | Umbralisib hydrochloride | FzM1 | Pamidronic acid | Fz7-21 | 4,5,6,7-Tetrabromo-1H-benzimidazole | JNJ-6204 | LGK974 | NSC668036 | CK2-IN-1 | JW67 | PF-5006739 | Ipafricept | TA-01 | Ellagic acid | EGFR-IN-57 | Ipivivint | WIC1 | AMG-548 hydrochloride | CKI-7 free base | SR-1277 | JW74 | IQ 1 | Heparan Sulfate | CK2α-IN-1 | L-Quebrachitol | NCC007 | Emodin-d4 | ETC-159 | HLY78
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货号: HY-13912
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