CXCR

ML339 a selective inhibitor of CXCR6(IC50 = 140 nM) with no response when screened against CXCR5 and CXCR4.

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.

SB225002 is a potent and selective CXCR2 antagonist inhibiting interleukin IL-8 binding to CXCR2.

JMS-17-2 is a potent and selective antagonist of CX3CR1 (IC50: 0.32 nM).

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

Mavorixafor (AMD-070) is an effective and selective antagonist of CXCR4, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells (IC50 = 1 nM) and PBMCs (IC50 = 9 nM).

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a 16-1 expression.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

ACT-1004-1239 is an orally active, selective, and potent CXCR7 antagonist with immune-modulatory and myelin-promoting effects. It can be used to study inflammatory demyelinating diseases.

Danirixin (GSK1325756) is a potent antagonist of CXCR2 that inhibits IL-8 binding to CXCR2 (IC50: 12.5 nM).

Mogamulizumab (KW-0761) is a monoclonal antibody targeting T cell CC chemokine receptor 4. It exhibits anticancer activity by eliminating tumor cells through antibody-dependent cytotoxicity (ADCC) and can be used in the study of cancer, adult T-cell leukemia lymphoma (ATLL), and cutaneous T-cell lymphoma (CTCL).

CXCR7 antagonist-1 is a specific antagonist of the binding of the SDF-1 chemokine or I-TAC to the chemokine receptor CXCR7. CXCR7 antagonist-1 prevents tumor cell proliferation and tumor formation and can be used in studies about inflammatory diseases.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

Ly2510924 acetate is an potent and selective CXCR4 antagonist. It prevents the binding of SDF-1 to CXCR4 with an IC50 of 0.079 nM.

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

Ulocuplumab (BMS-936564) is a fully human anti-CXCR4 IgG4 antibody.Ulocplumab exhibits antitumor activity in acute myeloid leukemia (AML), non-Hodgkin's lymphoma (NHL), and multiple myeloma transplantation models.Ulocplumab inhibits the migration of chronic lymphocytic leukemia (CLL) cells under CXCR4 activation, induces apoptosis, and inhibits the growth and migration of cancer cells. Ulocplumab inhibits CXCL12-mediated chronic lymphocytic leukemia (CLL) cell migration in response to CXCR4 activation and induces apoptosis.)

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

Reparixin (Repertaxin) is a potent inhibitor of both CXCL8 receptors CXCR1 2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).

Baohuoside I (Icariside-II) is a component of Epimedium koreanum, exhibits anti-inflammatory activity and anti-osteoporosis activities.

Eldelumab (BMS-936557) is a humanized anti-IP-10 IgG type 1 monoclonal antibody with inhibitory activity against CXCL10. It has anti-inflammatory properties, selectively binds to CXCL10, and can be used in the study of rheumatoid arthritis, ulcerative colitis, and Crohn's disease.

AZD-5069 is an chemokine receptor 2 antagonist (CXCR2; IC50 = 0.79 nM).

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

UNBS5162 (UNBS-5162) is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers.

Delmetacin (Demethacin) is a non-steroidal anti-inflammatory compound with anti-inflammatory and analgesic activity and inhibitory effects on the CXC chemokine receptor CXCR1.

FC131 TFA (606968-52-9 free base) (FC131 TFA) is an antagonist of CXCR4 that inhibits the binding of [125I] -sdf-1 to CXCR4(IC50 : 4.5 nM ), and has anti-hiv activity.

MSX-130 is CXCR4 Antagonist.

SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.

Ac-Pro-Gly-Pro-OH is an acetyl-modified tripeptide compound that acts as a CXCR2 agonist, exhibiting bactericidal and anti-inflammatory activities. It inhibits apoptosis of immune cells, suppresses the production of pro-inflammatory cytokines, and has been utilized in studies of sepsis and lung inflammation.

Artemotil (SM-227) is a new, fast-acting antimalarial drug.

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).

MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4 CXCL12 actions(IC50 = 10 nM).

VUF-11222 is a CXCR3 nonmimetic peptide agonist that induces gliosis.VUF 11222 has been used in the study of retinal inflammation.

IT1t dihydrochloride inhibits CXCL12 CXCR4 interaction with IC50 of 2.1 nM. IT1t dihydrochloride is an antagonist of CXCR4.

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1 2 (CXCR1 2) activation inhibitor.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

VUF11207 fumarate is an agonist of CXCR7 and a high-potency ligand of CXCR7 (pKi: 8.1).

rac-NBI-74330 is an effective and selective CXCR3 antagonist.

MSX-127 elicites positive response in peptide CXCR4.

WZ811 is a novel and effective small molecular CXCR4 antagonist (EC50: 0.3 nM).

ALX 40-4C acetate is a CXCR4 inhibitor of the chemokine receptor (Ki = 1 μM) and suppresses the replication of X4 strains of HIV-1. ALX 40-4C acetate is an antagonist of the APJ receptor (IC50 = 2.9 μM).