| 产品描述: | CXCR4 选择性抑制剂 | 激动剂 | 拮抗剂;CXCR4 Selective Inhibitors | Agonists | Antagonists;产品介绍: MSX-122是一种新型的CXCR4部分拮抗剂,IC50约为10 nM。;InformationMSX-122 is a novel small molecule and partialCXCR4antagonist (IC50~10 nM).TargetsCXCR4 ~10 nMIn vitroMSX-122 is also incapable of blocking the binding of 125I-labeled CXCL12 to CXCR4. MSX-122 appears to be insufficiently large to block all binding sites between CXCR4 and CXCL12. MSX-122 blocks certain CXCR4 functions via binding to the CXCL12-binding site and interfering with CXCR4/CXCL12-mediated signaling. MSX-122 can intervene in the Gαi-signaling pathway (cAMP modulation), but not the Gq-pathway (calcium flux).In vivoMSX-122 blocks bleomycin-induced lung fibrosis involving chemotaxis and homing of CXCR4-positive mesenchymal progenitor cells into the lungs. MSX-122 exhibits anti-inflammatory activity in a carrageenan-induced paw edema model. MSX-122 blocks lung metastasis of breast cancer and SCCHN, and liver metastasis of uveal melanoma in vivo.Cell Research(from reference)Cell lines:MDA-MB-231 cells Concentrations:1, 10, 100, and 1000 nM Incubation Time:15 mins |
| 体内研究: |
MSX-122 (10 mg/kg, i.p.) blocks inflammation induced by carrageenan and lung fibrosis induced by bleomycin in mice. MSX-122 (4 mg/kg, i.p., daily) blocks metastasis in an experimental animal model of breast cancer metastasis. Furthermore, MSX-122 (10 mg/kg i.p., daily) significantly decreases the numbers of hepatic micrometastases. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.421 ml |
17.103 ml |
34.207 ml |
| 5 mM |
0.684 ml |
3.421 ml |
6.841 ml |
| 10 mM |
0.342 ml |
1.71 ml |
3.421 ml |
| 50 mM |
0.068 ml |
0.342 ml |
0.684 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。 |