CXCR
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
CXCR产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8947New |
SX-682SX-682 是一种口服活性的 CXCR1 和 CXCR2 的小分子变构抑制剂，可以阻止肿瘤MDSC募集并增强T细胞活化和抗肿瘤免疫力。 |
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| S3951 |
Tannic acidTannic acid (Gallotannic acid) 是一种多酚化合物，是一种具有抗血管生成，抗炎和抗肿瘤活性的 CXCL12/CXCR4 的抑制剂。 |
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| S8640 |
Reparixin (Repertaxin)Reparixin (Repertaxin) 是一种有效且特异性的 CXCR1 抑制剂，IC50值为1 nM。Reparixin (Repertaxin) 可抑制 CXCL8 诱导的PMN迁移(IC50 = 1 nM)以及CXCL1和CXCL2诱导的啮齿动物PMN趋化性。Repertaxin 还可抑制人PMN对CXCL1的反应，其与 CXCR2 相互作用(IC50 = 400 nM)。 |
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| S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (AMD3100, JM 3100) 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。Plerixafor 可应用为抗HIV的药物。 |
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, JM 3100) 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。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。 |
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。 |
Gelatin degradation by COR-L23 (f) cells treated with 1 μM PF-573228 and 1 μM WZ811. Histograms showing percentages of degraded gelatin areas relative to the cell volume for each cell line are presented together with representative images. Merged channels show fluorescent gelatin (green), actin (red) and nuclei (blue) staining; dark areas represent spots of degraded gelatin. Scale bar = 100 μm. |
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| S8505 |
LY2510924LY2510924是一种有效的、选择性的CXCR4拮抗剂，特异性地阻止SDF-1与CXCR4的结合，IC50为0.079 nM；抑制SDF-1诱导的GTP结合，Kb值为0.38 nM。 |
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| S6645 |
AZD5069AZD5069是新型的CXCR2拮抗剂，它能抑制CXCL8与CXCR2的结合，pIC50值为8.8；抑制CXCL8与CXCR1结合，pIC50为6.5。 |
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| S9725New |
Balixafortide (POL6326)Balixafortide (POL6326) 是一种口服可生物利用的肽类 CXC chemokine receptor 4 (CXCR4) 的拮抗剂。 |
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| S9665New |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一种 CXCR4 的拮抗剂，IC50值约为1 nM。BL-8040 通过改变的miR-15a/16-1的表达，下调 ERK、BCL-2、MCL-1 和 cyclin-D1，诱导AML胚的凋亡。 |
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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。 |
SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05). |
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| S6620 |
Danirixin (GSK1325756)Danirixin (GSK1325756)是高亲和力的选择性CXCR2拮抗剂，抑制CXCL8 (IL-8)结合的IC50值为12.5 nM。 |
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| S8813 |
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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| S6617 |
MSX-122MSX-122是一种新型的CXCR4部分拮抗剂，IC50约为10 nM。 |
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| S4785 |
Nicotinamide N-oxideNicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. Nicotinamide N-oxide is novel, potent, and selective antagonists of the CXCR2 receptor. |
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| S8506 |
SCH-527123SCH-527123是有效的、具有口服生物利用度的CXCR2/CXCR1拮抗剂，IC50分别为2.6 nM和36 nM。 |
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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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| S8869 |
UNBS5162UNBS5162是CXCL趋化因子表达的拮抗剂，在一系列人类癌细胞包括恶性胶质瘤(Hs683和U373MG)、结肠直肠癌（HCT-15和LoVo）、乳腺癌细胞（MCF-7）中具有细胞毒性，IC50范围为0.5-5 μM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8947New |
SX-682SX-682 是一种口服活性的 CXCR1 和 CXCR2 的小分子变构抑制剂，可以阻止肿瘤MDSC募集并增强T细胞活化和抗肿瘤免疫力。 |
||
| S3951 |
Tannic acidTannic acid (Gallotannic acid) 是一种多酚化合物，是一种具有抗血管生成，抗炎和抗肿瘤活性的 CXCL12/CXCR4 的抑制剂。 |
||
| S8640 |
Reparixin (Repertaxin)Reparixin (Repertaxin) 是一种有效且特异性的 CXCR1 抑制剂，IC50值为1 nM。Reparixin (Repertaxin) 可抑制 CXCL8 诱导的PMN迁移(IC50 = 1 nM)以及CXCL1和CXCL2诱导的啮齿动物PMN趋化性。Repertaxin 还可抑制人PMN对CXCL1的反应，其与 CXCR2 相互作用(IC50 = 400 nM)。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (AMD3100, JM 3100) 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。Plerixafor 可应用为抗HIV的药物。 |
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.
|
|
| S8030 |
Plerixafor (AMD3100)Plerixafor (AMD3100, JM 3100) 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。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。 |
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.
|
|
| S2912 |
WZ811WZ811是一种高效的，竞争性的CXCR4拮抗剂，EC50为0.3 nM。 |
Gelatin degradation by COR-L23 (f) cells treated with 1 μM PF-573228 and 1 μM WZ811. Histograms showing percentages of degraded gelatin areas relative to the cell volume for each cell line are presented together with representative images. Merged channels show fluorescent gelatin (green), actin (red) and nuclei (blue) staining; dark areas represent spots of degraded gelatin. Scale bar = 100 μm. |
|
| S8505 |
LY2510924LY2510924是一种有效的、选择性的CXCR4拮抗剂，特异性地阻止SDF-1与CXCR4的结合，IC50为0.079 nM；抑制SDF-1诱导的GTP结合，Kb值为0.38 nM。 |
||
| S6645 |
AZD5069AZD5069是新型的CXCR2拮抗剂，它能抑制CXCL8与CXCR2的结合，pIC50值为8.8；抑制CXCL8与CXCR1结合，pIC50为6.5。 |
||
| S9725New |
Balixafortide (POL6326)Balixafortide (POL6326) 是一种口服可生物利用的肽类 CXC chemokine receptor 4 (CXCR4) 的拮抗剂。 |
||
| S9665New |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) 是一种 CXCR4 的拮抗剂，IC50值约为1 nM。BL-8040 通过改变的miR-15a/16-1的表达，下调 ERK、BCL-2、MCL-1 和 cyclin-D1，诱导AML胚的凋亡。 |
||
| S2879 |
AMD3465 hexahydrobromideAMD3465是一种单一大环类CXCR4的拮抗剂。 |
||
| 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。 |
SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05). |
|
| S6620 |
Danirixin (GSK1325756)Danirixin (GSK1325756)是高亲和力的选择性CXCR2拮抗剂，抑制CXCL8 (IL-8)结合的IC50值为12.5 nM。 |
||
| S8813 |
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。 |
||
| S6617 |
MSX-122MSX-122是一种新型的CXCR4部分拮抗剂，IC50约为10 nM。 |
||
| S4785 |
Nicotinamide N-oxideNicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. Nicotinamide N-oxide is novel, potent, and selective antagonists of the CXCR2 receptor. |
||
| S8506 |
SCH-527123SCH-527123是有效的、具有口服生物利用度的CXCR2/CXCR1拮抗剂，IC50分别为2.6 nM和36 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8869 |
UNBS5162UNBS5162是CXCL趋化因子表达的拮抗剂，在一系列人类癌细胞包括恶性胶质瘤(Hs683和U373MG)、结肠直肠癌（HCT-15和LoVo）、乳腺癌细胞（MCF-7）中具有细胞毒性，IC50范围为0.5-5 μM。 |
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