CXCR
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S3951 | Tannic acid | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S8640 | Reparixin (Repertaxin) | <1 mg/mL | 56 mg/mL | 56 mg/mL |
| S3013 | Plerixafor 8HCl (AMD3100 8HCl) | 100 mg/mL | <1 mg/mL | <1 mg/mL |
| S8030 | Plerixafor (AMD3100) | 3 mg/mL | <1 mg/mL | 100 mg/mL |
| S2912 | WZ811 | <1 mg/mL | 30 mg/mL | <1 mg/mL |
| S2879 | AMD3465 hexahydrobromide | 98 mg/mL | 2 mg/mL | <1 mg/mL |
| S7651 | SB225002 | <1 mg/mL | 70 mg/mL | 3 mg/mL |
| S8813 | LIT-927 | <1 mg/mL | 66 mg/mL | <1 mg/mL |
| S8309 | ATI-2341 | <1 mg/mL | 100 mg/mL | 2 mg/mL |
特异性亚型抑制剂
- CXCR抑制剂（9）
- 新CXCR产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3951New |
Tannic acidTannic acid, a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity. |
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| S8640 |
Reparixin (Repertaxin)Reparixin (Repertaxin)是人类和大鼠CXCR1/R2激活的抑制剂。它还可以抑制人类CXCL8受体的激活。 |
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| S3013 |
Plerixafor 8HCl (AMD3100 8HCl)Plerixafor 8HCl (AMD3100 8HCl)是Plerixafor的盐酸盐，是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。 |
BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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| S8030 |
Plerixafor (AMD3100)Plerixafor (AMD3100)是一种趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导的趋化性，无细胞试验中IC50分别为44 nM和5.7 nM。 |
BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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| S2912 |
WZ811WZ811是一种高效的，竞争性的CXCR4拮抗剂，EC50为0.3 nM。 |
a. Gelatin degradation by NCI-H460/R and COR-L23 cells treated with DOX, PF-573228, WZ811 and their combinations for 24 h. Images were captured using a 20× objective on a fluorescence microscope and representative examples are presented on the left part of the panel. At least 100 cells were analyzed per experiment. All experiments were performed at least three times. Merged channels show fluorescent gelatin (green), actin (red) and nuclei (blue) staining; dark areas represent spots of degraded gelatin. Scale bar = 100 μm. Corresponding histograms for each cell line are presented in the right part of the panel showing percentages of degraded gelatin areas relative to the cell volume. Each bar represents mean value ± S.E. * indicates p < 0.05 compared to untreated control cells; # indicates p < 0.05 compared to cells treated with PF-573228; $ indicates p < 0.05 compared to cells treated with WZ811.
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| S2879 |
AMD3465 hexahydrobromideAMD3465是一种单一大环类CXCR4的拮抗剂。 |
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| S7651 |
SB225002SB225002是一种强效的选择性CXCR2拮抗剂，抑制白介素IL-8与CXCR2的结合，IC50为22 nM，选择性比其它测试的7-TMRs高150多倍。 |
(G) Concentration-dependent inhibition of cell proliferation in SKOV3 cells (* P ≤ 0.005) treated with SB225002 (0.625, 1.25, 2.5 and 5 μM) for 2 days was revealed using XTT cell proliferation assay. (H) Western blot analysis confirmed that TAK1/NFκB signaling was inhibited dose-dependently in SKOV3 cells upon treatment with SB225002 (1.25 and 2.5 μM) as compared with untreated control.
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| S8813New |
LIT-927LIT-927是一种新型的CXCL12中性配体，抑制CXCL2和德州红染料的结合，Ki值为267 nM。它对CXCL12具有高选择性。 |
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| S8309 |
ATI-2341ATI-2341，一种靶向C-X-C 4型趋化因子受体（CXCR4）的肽段，是一个变构受体激动剂，能够激活异源三聚体G蛋白（Gi）、抑制cAMP生成以及诱导钙动员。 |
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