CXCR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	CXCR1	CXCR2	CXCR4	Other
A10913	Plerixafor 8HCl			**	CXCL12-mediated chemotaxis
A13074	Plerixafor			**	CXCL12-mediated chemotaxis
A12588	WZ811			****
A14209	SB225002		***
A16351	ATI-2341			*
A14997	AMD-070 HCl			***
A15234	SCH 563705	****	***
A14209	SB225002		***
A11555	SCH-527123 (Navarixin)	**	***
A12383	Reparixin	****	**		CXCL8
A12596	MSX-122			***
A11315	AMD 070			***

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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CXCR2-IN-1

Catalog No. A12649
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CXCR2 激动剂

CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. 了解更多

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PS372424

Catalog No. A19421
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Human CXCR3 拮抗剂

PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM. 了解更多

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Kynurenic acid

Catalog No. A16581
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GPR35/CXCR8 拮抗剂

Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. 了解更多

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USL311

Catalog No. A18778
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CXCR4 拮抗剂

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. 了解更多

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MSX-130

Catalog No. A17150
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CXCR4 拮抗剂

MSX-130是CXCR4拮抗剂。了解更多

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NSC-23026

Catalog No. A17151
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CXCR4 receptor modulator

NSC-23026是CXCR4受体调节剂。了解更多

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ATI-2341

Catalog No. A16351
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CXCR4 激动剂

ATI-2341是针对C-X-C趋化因子受体4型（CXCR4）（EC50 = 194 nM）的pepducin，是一种变构激动剂，可激活抑制性异三聚体G蛋白（Gi），从而促进cAMP生成的抑制并诱导钙动员。了解更多

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UNBS5162

Catalog No. A15439
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CXCL chemokines 拮抗剂

UNBS5162是一种新型萘二甲酰亚胺，可降低实验性前列腺癌中CXCL趋化因子的表达。9种癌细胞系的平均抗增殖活性IC50值为17.9 uM；UNBS3157的水解产物。了解更多

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AMD-070 HCl

Catalog No. A14997
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CXCR4 拮抗剂

在CXCR4 125I-SDF抑制结合试验中，AMD-070 HCl是一种有效的选择性CXCR4拮抗剂，IC50值为13 nM，抑制T-4型HIV-1（NL4.3株）在MT-4细胞中的复制和PBMC。了解更多

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Reparixin L-lysine salt

Catalog No. A15219
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CXCL8 receptor 抑制剂

Reparixin L-lysine salt是CXCL8受体的抑制剂，也抑制CXCR1和CXCR2的活化，已显示在各种损伤模型中减弱了炎症反应。了解更多

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SB225002

Catalog No. A14209
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CXCR2 拮抗剂

SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。了解更多

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Plerixafor 8HCl (DB06809)

Catalog No. A10913
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CXCR4 拮抗剂

Plerixafor 8HCl (DB06809)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。了解更多

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- Mei Zheng, .et al. CXCL12 inhibits hair growth through CXCR4, Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. Bone marrow cell homing to sites of acute tibial fracture: 89Zr-oxine cell labeling with positron emission tomographic imaging in a mouse model, EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. Bone marrow cell trafficking analyzed by 89Zr-oxine positron emission tomography in a murine transplantation model, Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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AMD 070

Catalog No. A11315
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CXCR4 拮抗剂

AMD 070是CXCR4趋化因子受体拮抗剂。了解更多

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- Uchida D, .et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells, Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. Enhancement of the CXCL12/CXCR4 axis due to acquisition of resistance in pancreatic cancer: effect of CXCR4 antagonists, BMC Cancer, 2016, 16: 305 PMID: 27175473
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AMD 3465 Hexahydrobromide

Catalog No. A11953
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CXCR4 拮抗剂

AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。了解更多

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- Kentaro Suzuki, .et al. C-terminal-modifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
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SRT3109

Catalog No. A11097
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CXCR2 ligand

SRT3109是一种CXCR2配体，用于治疗趋化因子介导的疾病和状况。了解更多

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WZ811

Catalog No. A12588
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CXCR4 拮抗剂

WZ811是4型C-X-C趋化因子受体（CXCR4）拮抗剂（EC50 = 0.3 nM）。在体外抑制CXCR4/基质细胞衍生因子1（SDF-1）介导的cAMP调节（EC50 = 1.2 nM）。了解更多

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MSX-122

Catalog No. A12596
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CXCR4 抑制剂

MSX-122是口服可生物利用的CXCR4抑制剂（IC50 =?10 nM），具有潜在的抗肿瘤和抗病毒活性。CXCR4抑制剂MSX-122与趋化因子受体CXCR4结合，阻止基质衍生因子-1（SDF-1）与CXCR4受体和受体激活结合，这可能导致肿瘤细胞增殖和迁移减少。了解更多

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SRT3190

Catalog No. A11577
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SIRT1 activator

SRT3190是一种强效cxcr2配体。了解更多

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Reparixin

Catalog No. A12383
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CXCL8/CXCR1/2 抑制剂

Reparixin是两种CXCL8受体CXCR1/2的有效抑制剂，它抑制CXCR2介导的细胞迁移（IC50 = 100 nM），而它强烈地阻断CXCR1介导的趋化性（IC50 = 1 nM）。了解更多

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- Naour AL, .et al. Tumor cells educate mesenchymal stromal cells to release chemoprotective and immunomodulatory factors, J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. N-acetyl cysteine improves the effects of corticosteroids in a mouse model of chlorine-induced acute lung injury, Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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AMD3100 (Plerixafor)

Catalog No. A13074
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CXCR4 拮抗剂

AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。了解更多

Product Citations (11)

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- Hitoshi Maeda, .et al. Cell-penetrating albumin enhances the sublingual delivery of antigens through macropinocytosis, Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. Brain vascular damage-induced lymphatic ingrowth is directed by Cxcl12b/Cxcr4a, Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. Effects of local vs systemic administration of CXCR4 inhibitor AMD3100 on orthodontic tooth movement in rats, Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. Positive effects of selenium supplementation on selenoprotein S expression and cytokine status in a murine model of acute liver injury, J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. Stromal cell-derived factor 1 (SDF1) attenuates platelet-derived growth factor-B (PDGF-B)-induced vascular remodeling for adipose tissue expansion in obesity, Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. Role of Prx1-expressing skeletal cells and Prx1-expression in fracture repair, Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. C-terminal?Cmodifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. Cell-penetrating mechanism of intracellular targeting albumin: Contribution of macropinocytosis induction and endosomal escape, J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. LPS-induced CXCR7 expression promotes gastric Cancer proliferation and migration via the TLR4/MD-2 pathway, Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. The role of conventional antibodies targeting the CD4 binding site and CD4-induced epitopes in the control of HIV-1 CRF01_AE viruses, Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. Microbe-dependent lymphatic migration of neutrophils modulates lymphocyte proliferation in lymph nodes, Nat Commun, 2015, 6: 7139 PMID: 25972253
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SCH-527123 (Navarixin)

Catalog No. A11555
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CXCR1/CXCR2 拮抗剂

SCH-527123 (Navarixin)是人CXCR1和CXCR2受体的强效选择性拮抗剂，IC50分别为42 nM和3 nM。了解更多

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- Ruijie Zhang, .et al. Combined inhibition of IL-6 and IL-8 pathways suppresses ovarian cancer cell viability and migration and tumor growth, Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. Inhibition of interleukin 8/C-X-C chemokine receptor 1,/2 signaling reduces malignant features in human pancreatic cancer cells, Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. Blocking Interleukin-6 and Interleukin-8 Signaling Inhibits Cell Viability, Colony-forming Activity, and Cell Migration in Human Triple-negative Breast Cancer and Pancreatic Cancer Cells, Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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SB265610

Catalog No. A14195
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CXCR2 拮抗剂

SB265610是CXCR2 (Kd = 2.51 nM)的非肽变构反向激动剂，通过与不同于激动剂结合位点的区域结合来防止受体活化。它不与相关CXCR1受体结合。在体外和高氧诱导肺损伤的大鼠模型中，它已被证明能防止中性粒细胞趋化性。了解更多

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AZD-5069

Catalog No. A15941
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CXCR2 拮抗剂

AZD-5069是一种有效的选择性CXCR2拮抗剂，具有抑制COPD患者中性粒细胞向气管迁移的潜能。了解更多

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SCH 563705

Catalog No. A15234
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CXCR2/CXCR1 拮抗剂

SCH 563705是有效的双重CXCR2（IC50 = 1.3 nM)/CXCR1（IC50 = 7.3 nM）拮抗剂。了解更多

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GPR35 agonist 1

Catalog No. A12462
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GPR35/CXCR8 agonist

GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. 了解更多

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Kynurenic acid sodium

Catalog No. A20000
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GPR35/CXCR8 agonist

Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8. 了解更多

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AMG 487

Catalog No. A21162
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CXCR3 antagonist

AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively. 了解更多

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SCH 546738

Catalog No. A21554
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CXCR3 antagonist

SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments. 了解更多

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AMG 487 S-enantiomer

Catalog No. A21874
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CXCR3 antagonist

AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3. 了解更多

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NBI-74330

Catalog No. A21158
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CXCR3 antagonist

NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively. 了解更多

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