1. Signaling Pathways
  2. GPCR/G Protein
    Immunology/Inflammation
  3. CXCR

CXCR

CXCR

CXC chemokine receptors; C-X-C motif chemokine receptors

CXCRs (CXC chemokine receptors) are integral membrane proteins that specifically bind and respond to cytokines of the CXC chemokine family. They represent one subfamily of chemokine receptors, a large family of G protein-linked receptors that are known as seven transmembrane (7-TM) proteins, since they span thecell membrane seven times. There are currently seven known CXC chemokine receptors in mammals, named CXCR1 through CXCR7. CXCR1 and CXCR2 are closely related receptors that recognize CXC chemokines that possess an E-L-R amino acid motif immediately adjacent to their CXC motif. CXCR3 is expressed predominantly on T lymphocytes. CXCR4 is the receptor for a chemokine known as CXCL12 (or SDF-1) and, as with CCR5, is utilized by HIV-1 to gain entry into target cells. The chemokine receptor CXCR5 is selectively expressed on B cells and is involved in lymphocyte homing and the development of normal lymphoid tissue. CXCR6 was formerly called three different names (STRL33, BONZO, and TYMSTR) before being assigned CXCR6 based on its chromosomal location and its similarity to other chemokine receptors in its gene sequence. CXCR7 was originally called RDC-1 (an orphan receptor) but has since been shown to cause chemotaxis in T lymphocytes in response to CXCL12 (the ligand for CXCR4) prompting the renaming of this molecule as CXCR7.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10046
    Plerixafor
    Antagonist 99.90%
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
    Plerixafor
  • HY-16711
    SB225002
    Antagonist 99.87%
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
    SB225002
  • HY-15319
    AMG 487
    Inhibitor 99.80%
    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.
    AMG 487
  • HY-15251
    Reparixin
    Inhibitor 99.99%
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin
  • HY-100806
    Kynurenic acid
    99.21%
    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.
    Kynurenic acid
  • HY-P4111A
    Peptide R TFA
    Antagonist 98.34%
    Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research.
    Peptide R TFA
  • HY-10011A
    (S)-SCH 563705
    Antagonist 99.94%
    (S)-SCH 563705 is a S-enantiomer of SCH 563705. SCH 563705 (compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
    (S)-SCH 563705
  • HY-10011B
    (Rac)-SCH 563705
    Antagonist 99.78%
    (Rac)-SCH 563705 is a racemic mixture of SCH 563705 (HY-10011). SCH 563705 (compound 16) is a potent and orally active CXCR2 and CXCR1 antagonist with IC50 values ​​of 1.3 nM and 7.3 nM and Ki values ​​of 1 nM and 3 nM, respectively.
    (Rac)-SCH 563705
  • HY-50912
    Plerixafor octahydrochloride
    Antagonist 99.09%
    Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
    Plerixafor octahydrochloride
  • HY-10198
    Navarixin
    Antagonist 98.90%
    Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
    Navarixin
  • HY-13848
    AZD8797
    99.54%
    AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
    AZD8797
  • HY-19855
    AZD-5069
    Antagonist 99.91%
    AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
    AZD-5069
  • HY-13406
    TAK-779
    Antagonist 99.73%
    TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
    TAK-779
  • HY-P0171
    Motixafortide
    Antagonist 99.88%
    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
    Motixafortide
  • HY-142617
    ACT-1004-1239
    Antagonist 99.80%
    ACT-1004-1239 is a potent, selective, orally active CXCR7 antagonist with an IC50 value of 3.2 nM.
    ACT-1004-1239
  • HY-N0011
    Baohuoside I
    Inhibitor 99.96%
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
    Baohuoside I
  • HY-122197
    ML339
    Antagonist 99.88%
    ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5CXCR4CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research.
    ML339
  • HY-50101A
    Mavorixafor trihydrochloride
    Antagonist 99.75%
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome.
    Mavorixafor trihydrochloride
  • HY-119339
    SX-682
    Inhibitor 99.67%
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
    SX-682
  • HY-111793A
    NUCC-390 dihydrochloride
    Agonist 98.19%
    NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.
    NUCC-390 dihydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

CXCR

CXCR1

CXCR2

CXCR3

CXCR4

CXCR7

CXCR6

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Please try each isoform separately.

CXCR Inhibitors, Agonists, Antagonists, Activators & Modulators
Product NameCXCRCXCR1CXCR2CXCR3CXCR4CXCR7CXCR6Purity    
Plerixafor    
125I-CXCL12-CXCR4, IC50: 44 nM
  99.90%
SB225002  
125I-IL-8-CXCR2, IC50: 22 nM (in CHO cell membrane)
    99.87%
AMG 487   
125I-IP10-CXCR3, IC50: 8 nM
125I-ITAC-CXCR3, IC50: 8.2 nM
   99.80%
Reparixin 
CXCR1wt, IC50: 5.6 nM (in L1.2 cells)
CXCR1Ile43Val, IC50: 80 nM (in L1.2 cells)
CXCR1, IC50: 1 nM (in cells)
CXCR2, IC50: ∼100 nM (in cells)
    99.99%
Peptide R TFA    
CXCR4
  98.34%
Plerixafor octahydrochloride    
125I-CXCL12-CXCR4, IC50: 44 nM
  99.09%
Navarixin 
Cynomolgus CXCR1, Kd: 41 nM
125I-CXCL8-CXCR1, IC50: 43 nM
Mouse CXCR2, Kd: 0.2 nM
Rat CXCR2, Kd: 0.2 nM
Cynomolgus CXCR2, Kd: 0.08 nM
125I-CXCL8-CXCR2, IC50: 0.97 nM
    98.90%
AZD8797  
125I-IL-8-CXCR2, Ki: 2800 nM (in HEK293S cells)
    99.54%
AZD-5069  
125I-IL-8-CXCR2
    99.91%
TAK-779   
mCXCR3, IC50: 369 nM (in PBMCs)
   99.73%
Motixafortide    
CXCR4, IC50: ~1 nM
  99.88%
ACT-1004-1239     
CXCR7
 99.80%
Baohuoside I    
CXCR4
  99.96%
ML339      
CXCR6, IC50: 140 nM
99.88%
Mavorixafor trihydrochloride    
125I-SDF-CXCR4, IC50: 13 nM
  99.75%
SX-682 
CXCR1
CXCR2
    99.67%
NUCC-390 dihydrochloride    
CXCR4
  98.19%
IT1t dihydrochloride    
CXCL12/CXCR4, IC50: 2.1 nM
  99.77%
SCH 546738   
Human CXCR3, Ki: 0.4 nM
   98.71%
LY2510924    
125I-SDF-1α-CXCR4, IC50: 79.7 pM
125I-SDF-1α-CXCR4, Ki: 49.5 pM
  99.73%
CXCR7 antagonist-1     
CXCR7
 99.85%
SB-265610  
CXCR2
    ≥99.0%
VUF11207 fumarate     
CXCR7, pKi: 8.1
 98.50%
Danirixin  
CXCL8-CXCR2, IC50: 12.5 nM
    98.88%
Reparixin L-lysine salt 
CXCR1wt, IC50: 5.6 nM (in L1.2 cells)
CXCR1Ile43Val, IC50: 80 nM (in L1.2 cells)
CXCR1, IC50: 1 nM (in cells)
CXCR2, IC50: ∼100 nM (in cells)
    99.66%
NBI-74330   
[125I]CXCL10-CXCR3, Ki: 1.5 nM (in CXCR3-CHO cell membranes)
[125I]CXCL11-CXCR3, Ki: 3.2 nM (in CXCR3-CHO cell membranes)
   98.57%
ACT-777991   
CXCR3
   99.86%
Ulocuplumab    
CXCR4
  99.90%
Nicotinamide N-oxide  
CXCR2
    99.85%
TC14012    
CXCR4, IC50: 19.3 nM (antagonist site)
CXCR7, EC50: 350 nM (agonist site)
 98.92%
PS372424 hydrochloride   
Human CXCR3
   ≥98.0%
Balixafortide TFA    
CXCR4, IC50: <10 nM
  99.78%
WZ811    
CXCR4, EC50: 0.3 nM
  99.80%
Elubrixin tosylate  
CXCR2
    99.78%
Ladarixin sodium 
CXCR1
CXCR2
    99.84%
CTCE-0214    
SDF-1α-CXCR4
  98.94%
CXCR2 antagonist 8  
CXCR2
    99.24%
SX-517 
CXCR1
CXCR2
    99.88%
Burixafor hydrobromide    
CXCR4
  ≥98.0%
AMD 3465 hexahydrobromide    
12G5 mAb-CXCR4, IC50: 0.75 nM (in SupT1 cells)
CXCL12AF647-CXCR4, IC50: 18 nM (in SupT1 cells)
  ≥98.0%
MSX-122    
CXCR4/CXCL12, IC50: ~10 nM
  98.92%
SCH 563705 
CXCR1, Ki: 3 nM
CXCR1, IC50: 7.3 nM
CXCR2, Ki: 1 nM
CXCR2, IC50: 1.3 nM
Mouse CXCR2, IC50: 5.2 nM
    99.86%
CXCR2-IN-1  
CXCR2, pIC50: 9.3
    99.54%
CXCR2-IN-2 
CXCR1, IC50: 3.8 μM
CXCR2, IC50: 5.2 nM
    99.52%
FC131 TFA    
125I-SDF-1-CXCR4, IC50: 4.5 nM
  99.89%
CTCE-9908    
CXCR4
  99.47%
CXCR7 antagonist-1 hydrochloride     
CXCR7
 99.41%
CXCR7 modulator 2     
CXCR7, Ki: 13 nM
 98.71%
ALX 40-4C Trifluoroacetate    
SDF-1-CXCR4, Ki: 1 μM
  
AMD 3465    
12G5 mAb-CXCR4, IC50: 0.75 nM (in SupT1 cells)
CXCL12AF647-CXCR4, IC50: 18 nM (in SupT1 cells)
  99.59%
USL311    
CXCR4
  99.97%
LIT-927    
CXCL12/CXCR4, Ki: 267 nM
  99.86%
UNBS5162
CXCL
      98.10%
AZD8309  
CXCR2, IC50: 4 nM
    99.98%
ACT-660602   
CXCR3, IC50: 204 nM
   99.86%
CXCR7 modulator 1     
CXCR7, Ki: 9 nM
 99.50%
AMG 487 (S-enantiomer)   
CXCR3
   99.94%
MSX-127    
CXCR4
  99.68%
SRT3190  
CXCR2
    99.77%
EPI-X4    
CXCR4, IC50: 8.6 μM
  99.21%
NUCC-390    
CXCR4
  98.40%
Mavorixafor hydrochloride    
125I-CXCL12-CXCR4, IC50: 13 nM
  99.10%
Elubrixin  
CXCR2
    
IT1t    
CXCL12/CXCR4, IC50: 2.1 nM
  
Peptide R    
CXCR4
  
CXCR3 antagonist 1   
CXCR3, IC50: 0.06 μM
   98.40%
ALX 40-4C    
SDF-1-CXCR4, Ki: 1 μM
  
PS372424   
Human CXCR3
   
Mavorixafor    
125I-SDF-CXCR4, IC50: 13 nM
  
MSX-130    
CXCR4
  98.00%
KRH-3955 hydrochloride    
SDF-1α-CXCR4, IC50: 0.61 nM
  
FC131    
125I-SDF-CXCR4, IC50: 4.5 nM
  
SRT3109  
CXCR2, pIC50: 8.2
    99.82%
Balixafortide    
CXCR4, IC50: <10 nM
  
AZ10397767  
CXCR2, IC50: 1 nM
    
CXCR4 antagonist 7    
CXCR4/CXCL12, IC50: 9.3 nM
  
CXCR4 antagonist 10    
CXCR4, IC50: 7.8 nM
  
CXCR2 antagonist 7  
CXCR2, IC50: 0.044 μM
    
BC-1485 
CXCR1
     
Hit 14    
12G5 mAb-CXCR4, IC50: 254 nM
  
CTCE-9908 TFA    
CXCR4
  
CXCR2 antagonist 6  
CXCR2, IC50: 0.43 μM
    
TC14012 TFA    
CXCR4, IC50: 19.3 nM (antagonist site)
CXCR7, EC50: 350 nM (agonist site)
 
Nicotinamide N-oxide (Standard)  
CXCR2
    
CXCR2 antagonist 5  
CXCR2, IC50: 0.013 μM
    
CXCR4 modulator-1    
CXCR4, EC50: 100 nM
  
CXCR4 antagonist 5    
CXCR4, IC50: 8.8 nM
  
CXCR4 antagonist 9    
CXCR4, IC50: 15 nM
  
CXCR4 antagonist 3    
CXCR4, IC50: 11 nM
  
CXCR4 antagonist 4    
CXCR4, IC50: 24 nM
  
VUF11207 TFA     
CXCR7, pKi: 8.1
 
TIQ-15    
CXCR4, IC50: 6 nM
  
ATI-2341    
CXCR4, EC50: 194 nM (in CCRF-CEM cells)
  
CCX662     
CXCR7
 
CXCR4 modulator-2    
CXCR4, IC50: 1.25 nM
  
CXCR4 antagonist 8    
CXCR4, IC50: 57 nM
  
Corydalmine  
CXCR2
    
Ac-Pro-Gly-Pro-OH  
CXCR2
    
CXCR4 antagonist 1    
CXCR4
  
VUF11418  
CXCR2
    
BAM-12P     
CXCR7, EC50: 175 nM
 
HF50731    
CXCR4, IC50: 19.8 nM
  
CXCR4-IN-3    
CXCR4, IC50: 3.2 nM
  
ICT5040    
CXCR4, IC50: 3.8 μM
  
RCP168    
CXCR4, IC50: 5 nM
  
CXCR2 antagonist 4  
CXCR2, IC50: 0.13 μM
    
CXCR4 antagonist 6    
CXCR4, IC50: 79 nM
  
KRH-1636    
CXCR4
  
VUF11207     
CXCR7, pKi: 8.1