产品描述: | XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation |
靶点: |
TNKS2:2 nM (IC50);TNKS1:5 nM (IC50);ARTD2:479 nM (IC50);ARTD1:5500 nM (IC50);PARP;Wnt/beta-catenin |
体内研究: |
XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo |
参考文献: |
1. Mohit Narwal, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9. 2. Nuha Almasoud, et al. Tankyrase inhibitor XAV-939 enhances osteoblastogenesis and mineralization of human skeletal (mesenchymal) stem cells. Sci Rep. 2020 Oct 7;10(1):16746. 3. Senxin Cai, et al. Mechanical stress reduces secreted frizzled-related protein expression and promotes temporomandibular joint osteoarthritis via Wnt/β-catenin signaling. Bone. 2022 Aug;161:116445. |
溶解性: |
DMSO : 15.62 mg/mL (50.01 mM; ultrasonic and warming and heat to 60°C) H2O : < 0.1 mg/mL (insoluble) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.202 ml |
16.01 ml |
32.019 ml |
5 mM |
0.64 ml |
3.202 ml |
6.404 ml |
10 mM |
0.32 ml |
1.601 ml |
3.202 ml |
50 mM |
0.064 ml |
0.32 ml |
0.64 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |