产品描述: | IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway. |
靶点: |
IC50: 180 nM (Wnt);Wnt/beta-catenin |
体外研究: |
Both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects in vitro. IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly. IWR-1 (10 μM) induces stabilization of β-catenin disruption complex. IWR-1 (10 μM) is added to the medium together with MIF, the size of cell colonies is extremely decreased, and that indicates the promoting effect of MIF on NSPC proliferation is inhibited by IWR-1 in any MIF concentration group. 2, 5 and 10 μM of IWR-1 significantly inhibits the proliferation of NSPC dose-dependently. IWR-1 inhibites the promoting effect of MIF on NSPC differentiation to neuron lineage. IWR-1 treatment in the presence of maximal stimulatory dose of FSH (0.5 ng/mL) results in a dose dependent inhibition of the stimulatory effect of FSH with > 75% inhibition observed at the maximal inhibitory dose of IWR-1 (1 µM). IWR-1 treatment partially reverses the FSH-induced inhibition of granulosa cell CARTPT mRNA expression[ |
参考文献: |
1. Lu J, et al. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. 2. Zhang X, et al. Macrophage migration inhibitory factor promotes proliferation and neuronal differentiation of neural stem/precursor cells through Wnt/β-catenin signal pathway. Int J Biol Sci. 2013 Nov 28;9(10):1108-20. 3. Gupta PS, et al. Regulation and Regulatory Role of WNT Signaling in Potentiating FSH Action during Bovine Dominant Follicle Selection. PLoS One. 2014 Jun 17;9(6):e100201. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.442 ml |
12.212 ml |
24.424 ml |
5 mM |
0.488 ml |
2.442 ml |
4.885 ml |
10 mM |
0.244 ml |
1.221 ml |
2.442 ml |
50 mM |
0.049 ml |
0.244 ml |
0.488 ml |
|
注意: |
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