产品描述: | MSX-122 (Q-122)是一种新型的CXCR4部分拮抗剂,IC50约为10 nM |
靶点: |
CXCR4:~10 nM;CXCR |
体外研究: |
MSX-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) |
体内研究: |
MSX-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 |
细胞实验: |
Cell lines: MDA-MB-231 cells Concentrations: 1, 10, 100, and 1000 nM Incubation Time: 15 mins Method: For binding affinity assay, MDA-MB-231 cells cultured in an 8-well slide chamber are preincubated with MSX-122 at 1, 10, 100, and 1000 nM. Then the cells are fixed with 4% formaldehyde and incubated with 50 nM biotinylated TN14003, and followed by Rhodamine staining. |
动物实验: |
Animal Models: Male C57BL/6 mice (age 5–6 weeks) Dosages: 10 mg/kg Administration: i.p. injection |
参考文献: |
1. Liang Z, et al. Development of a unique small molecule modulator of CXCR4. PLoS One. 2012, 7(4):e34038. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
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。 |