CXCR

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抑制剂选择性比较

特异性亚型抑制剂

CXCR产品

所有产品 CXCR抑制剂(3) CXCR拮抗剂(13) CXCR激动剂(1) CXCR调节剂(1)

目录号	产品描述	文献引用	实验数据
S8947^New	SX-682 SX-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 acid Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.
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。	Nat Protoc, 2020, 15(2):421-449 Biomed Pharmacother, 2020, 122:109693 J Exp Clin Cancer Res, 2019, 38(1):461
S3013	Plerixafor 8HCl (AMD3100 8HCl) Plerixafor 8HCl (AMD3100, JM 3100) 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。	Mol Oncol, 2020, 14(4):779-794 Int J Nanomedicine, 2020, 15:5701-5718 Biol Reprod, 2019, 101(1):102-111	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。	Cell Rep, 2020, 33(1):108221 Cell Death Dis, 2020, 11(8):707 Cell Chem Biol, 2020, 10.1016/j.chembiol.2020.01.010	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	WZ811 WZ811是一种高效的，竞争性的CXCR4拮抗剂，EC50为0.3 nM。	Cell Rep, 2020, 33(1):108221 Am J Physiol Lung Cell Mol Physiol, 2018, 315(3):L404-L421 J Cancer, 2018, 9(6):929-940	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	LY2510924 LY2510924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^New	AZD5069 AZD5069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。
S9665^New	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。
S8506^New	SCH-527123 SCH-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。
S6617^New	MSX-122 MSX-122是一种新型的CXCR4部分拮抗剂，IC50约为10 nM。
S2879	AMD3465 hexahydrobromide AMD3465是一种单一大环类CXCR4的拮抗剂。
S7651	SB225002 SB225002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。	Cell Death Dis, 2020, 11(8):707 Cell Oncol (Dordr), 2020, 10.1007/s13402-020-00554-0 PLoS One, 2020, 27;15(4):e0232230	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结合的IC50值为12.5 nM。	Theranostics, 2019, 9(18):5332-5346
S8813	LIT-927 LIT-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。
S4785	Nicotinamide N-oxide Nicotinamide 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.
S8309	ATI-2341 ATI-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。
S8869	UNBS5162 UNBS5162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

S8947^New

SX-682

SX-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 acid

Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.

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。

Nat Protoc,2020, 15(2):421-449

Biomed Pharmacother,2020, 122:109693

J Exp Clin Cancer Res,2019, 38(1):461

目录号	产品描述	文献引用	实验数据
S3013	Plerixafor 8HCl (AMD3100 8HCl) Plerixafor 8HCl (AMD3100, JM 3100) 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。	Mol Oncol, 2020, 14(4):779-794 Int J Nanomedicine, 2020, 15:5701-5718 Biol Reprod, 2019, 101(1):102-111	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。	Cell Rep, 2020, 33(1):108221 Cell Death Dis, 2020, 11(8):707 Cell Chem Biol, 2020, 10.1016/j.chembiol.2020.01.010	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	WZ811 WZ811是一种高效的，竞争性的CXCR4拮抗剂，EC50为0.3 nM。	Cell Rep, 2020, 33(1):108221 Am J Physiol Lung Cell Mol Physiol, 2018, 315(3):L404-L421 J Cancer, 2018, 9(6):929-940	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	LY2510924 LY2510924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^New	AZD5069 AZD5069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。
S9665^New	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。
S8506^New	SCH-527123 SCH-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。
S6617^New	MSX-122 MSX-122是一种新型的CXCR4部分拮抗剂，IC50约为10 nM。
S2879	AMD3465 hexahydrobromide AMD3465是一种单一大环类CXCR4的拮抗剂。
S7651	SB225002 SB225002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。	Cell Death Dis, 2020, 11(8):707 Cell Oncol (Dordr), 2020, 10.1007/s13402-020-00554-0 PLoS One, 2020, 27;15(4):e0232230	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结合的IC50值为12.5 nM。	Theranostics, 2019, 9(18):5332-5346
S8813	LIT-927 LIT-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。
S4785	Nicotinamide N-oxide Nicotinamide 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.

目录号	产品描述	文献引用	实验数据
S8309	ATI-2341 ATI-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

S8309

ATI-2341

ATI-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	UNBS5162 UNBS5162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

S8869