上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
IWP-2 纯度: 99.51%
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。
IWP-2 Chemical Structure
CAS No. : 686770-61-6
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IWP-2 相关产品
•相关化合物库:
- 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
生物活性 |
IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ[1][2]. |
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IC50 & Target |
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体外研究 (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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
466.60 |
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Formula |
C22H18N4O2S3 |
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CAS 号 |
686770-61-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMF : 12.5 mg/mL (26.79 mM; ultrasonic and warming and heat to 60°C) DMSO : 2 mg/mL (4.29 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
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参考文献 |
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Cell Assay [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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration |
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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